MedWorm.com provides a medical RSS filtering service. Over 6000 RSS medical sources are combined and output via different filters. This feed contains the latest items from the 'European Journal of Pharmacology' source. Sun, 21 Mar 2010 14:58:02 +0100 http://www.medworm.com/index.php?rid=3374905&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20230815%26dopt%3DAbstract Authors: Minai-Tehrani D, Fooladi N, Minoui S, Sobhani-Damavandifar Z, Aavani T, Heydarzadeh S, Attar F, Ghaffari M, Nazem H Scopolamine (hyoscine) is commonly used as an anticholinergic drug to relieve nausea, vomiting and dizziness of a motion sickness as well as recovery from anesthesia and surgery. Sucrase as a hydrolytic enzyme breaks down sucrose into its monomers, glucose and fructose. The aim of this study was to evaluate the effect of scopolamine on the activity and the structural changes of yeast sucrase. The results showed that binding of scopolamine to sucrase could inhibit the enzyme activity. A non-competitive inhibition was observed in different concentrations of scopolamine (0.6 to 3.6mM). The study by circular dichroism measurement in far-UV showed that the absolute en... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3374905 Fri, 12 Mar 2010 00:00:00 +0100 3374905 http://www.medworm.com/index.php?rid=3374907&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20226179%26dopt%3DAbstract Authors: Wang X, Stavchansky S, Kerwin SM, Bowman PD To determine the relationship between catechol ring modifications and the activity of caffeic acid phenethyl ester (CAPE) as a cytoprotective agent, six catechol ring-fluorinated CAPE derivatives were evaluated for their cytoprotective abilities, as well as for their antioxidant and heme oxygenase-1 (HO-1) inducing capacity in a human umbilical vein endothelial cell (HUVEC) model of oxidant stress. To ascertain the involvement of HO-1 induction in the cytoprotective effects of CAPE analogues, their ability to induce HO-1 at 20microM was determined by reverse transcriptase polymerase chain reaction, western blotting and the use of HO-1 inhibitor tin protoporphyrin IX. There was significant induction of HO-1 by CAPE derivatives. Inhibi... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3374907 Tue, 09 Mar 2010 00:00:00 +0100 3374907 http://www.medworm.com/index.php?rid=3374906&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20226180%26dopt%3DAbstract Authors: Munoz L, Ramsay EE, Manetsch M, Ge Q, Peifer C, Laufer S, Ammit AJ SB203580 is the prototypical p38 MAPK inhibitor; however it cannot be used clinically due to liver toxicity. We developed a structural analogue of SB203580 - ML3403 - with equal in vitro and ex vivo p38alpha MAPK inhibition as SB203580, but with reduced activity towards liver cytochrome P450 enzymes. In addition, we developed a selective p38alpha MAPK inhibitor - CP41. The aim of this study is to compare the anti-inflammatory activity of ML3403 and CP41, with SB203580. We compare and contrast the ability of the p38 MAPK inhibitors to repress tumour necrosis factor alpha (TNFalpha)-induced interleukin 6 (IL-6) and interleukin 8 (IL-8) mRNA expression and protein secretion from airway smooth muscle cells. We also... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3374906 Tue, 09 Mar 2010 00:00:00 +0100 3374906 http://www.medworm.com/index.php?rid=3363132&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20223232%26dopt%3DAbstract In this study two doses of etazolate were tested for cognitive effects in normally aged rats, using a complex spatial learning and memory task that emphasized two naturally occurring behaviors in rodents, foraging for food and returning large pieces of found food to a safe home location. Both etazolate doses completely prevented both (1) a foraging deficit that developed in untreated aged rats over the course of the test, as well as (2) a trial-specific deficit in memory for previously visited food locations that also developed over the course of the test in untreated aged rats. Both doses also significantly reduced a separate memory deficit for changing locations of the animals' home box, plus completely prevented a significant tendency for untreated aged animals to attempt entry into sim... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3363132 Mon, 08 Mar 2010 00:00:00 +0100 3363132 http://www.medworm.com/index.php?rid=3356495&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20206620%26dopt%3DAbstract Authors: Qi X, Okamoto Y, Murakawa T, Wang F, Oyama O, Ohkawa R, Yoshioka K, Du W, Sugimoto N, Yatomi Y, Takuwa N, Takuwa Y Therapeutic angiogenesis is a promising strategy for treating ischemia. The lysophospholipid mediator sphingosine-1-phosphate (S1P) acts on vascular endothelial cells to stimulate migration and tube formation, and plays the critical role in developmental angiogenesis. We developed poly(lactic-co-glycolic-acid) (PLGA)-based S1P-containing microparticles (PLGA-S1P), which are biodegradable and continuously release S1P, and studied the effects of PLGA-S1P on neovascularization in murine ischemic hindlimbs. Intramuscular injections of PLGA-S1P stimulated blood flow in C57BL/6 mice dose-dependently, with repeated administrations at a 3-day interval, rather than a singl... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3356495 Wed, 03 Mar 2010 00:00:00 +0100 3356495 http://www.medworm.com/index.php?rid=3356496&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20206157%26dopt%3DAbstract Authors: Mainzen Prince PS, Sathya B Lipids and lipoproteins play an important role in the pathology of myocardial infarction. This manuscript reports the preventive effect of quercetin on lipids, lipoproteins and electrocardiogram in isoproterenol treated cardiotoxic male Wistar rats. Quercetin (10mg/kg) was administered orally as pretreatment to Wistar rats daily for seven days. After pretreatment, rats were induced myocardial infarction by subcutaneous injection of isoproterenol (100mg/kg) at an interval of 24h for two days. Quercetin pretreatment significantly (P<0.05) lowered ST-segment elevation and decreased the levels of lipid peroxidation products in plasma and heart in isoproterenol treated cardiotoxic rats. Quercetin pretreatment also significantly (P<0.05) reduced the... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3356496 Tue, 02 Mar 2010 00:00:00 +0100 3356496 http://www.medworm.com/index.php?rid=3343006&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20202467%26dopt%3DAbstract Authors: Vayssettes-Courchay C, Ragonnet C, Camenen G, Félétou M, Cordi AA, Lavielle G, Verbeuren TJ Inflammation plays a major role in pathological conditions leading to cardiovascular events. Administration of lipopolysaccharide to animals decreases arterial blood flow, in contrast to the dilatations that occur in microvessels. The purpose of the present study was to determine whether or not lipopolysaccharide, in vivo, evokes arterial constriction and if so the underlying mechanisms. Rabbits were anaesthetized, blood pressure monitored and femoral artery diameter continuously recorded with an echotracking device. Lipopolysaccharide induced leucopenia, thrombocytopenia, acidosis and a progressive hypotension with a decrease in femoral artery diameter (-30.7+/-2.4 % after 3h... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3343006 Mon, 01 Mar 2010 00:00:00 +0100 3343006 http://www.medworm.com/index.php?rid=3331986&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20193676%26dopt%3DAbstract Authors: Awwad HO, Millman EE, Alpizar-Foster E, Moore RH, Knoll BJ The internalization of beta(2)-adrenoceptors after agonist activation results in a desensitized and phosphorylated receptor that either resensitizes by recycling to the cell surface or becomes degraded by postendocytic sorting to lysosomes. The duration and physiological effects of agonists therefore depend on beta(2)-adrenoceptor sorting, highlighting the importance of sorting signals. Dileucine motifs within other membrane proteins act as signals for endocytosis and/or postendocytic sorting, and the beta(2)-adrenoceptor has a dileucine motif within helix 8 that might play a role in efficient receptor recycling and/or downregulation. beta(2)-adrenoceptor internalization and sorting were studied in HEK293 cells stably ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3331986 Fri, 26 Feb 2010 00:00:00 +0100 3331986 http://www.medworm.com/index.php?rid=3331985&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20193677%26dopt%3DAbstract In conclusion, the present results provide evidence that 17beta-estradiol regulates the expression of muscarinic acetylcholine receptor subtypes and estrogen receptor alpha. The immediate replacement with estrogen seems critical to restore the expression of these receptors after hormonal deprivation. The understanding of the regulation of expression and intracellular signaling of the muscarinic acetylcholine receptor subtype M(1) and the estrogen receptor alpha may be helpful to elucidate the mechanisms involved in changes of cognitive function in postmenopausal women and in neurodegenerative diseases. PMID: 20193677 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3331985 Fri, 26 Feb 2010 00:00:00 +0100 3331985 http://www.medworm.com/index.php?rid=3331984&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20193678%26dopt%3DAbstract In this study, the effect of hypericin, a major active constituent of St. John's wort that is widely used in the treatment of depression, on the release of glutamate from nerve terminals purified from rat cerebral cortex was examined. Result showed that hypericin inhibited the release of glutamate evoked by 4-aminopyridine in a concentration-dependent manner. Further experiments revealed that hypericin-mediated inhibition of glutamate release (i) results from a reduction of vesicular exocytosis, not form an inhibition of Ca(2+)-independent efflux via glutamate transporter; (ii) is not due to an alternation of nerve terminal excitability; (iii) is associated with a decrease in presynaptic N- and P/Q-type voltage-dependent Ca(2+) channel activity; and (iv) appears to involve the suppression ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3331984 Fri, 26 Feb 2010 00:00:00 +0100 3331984 http://www.medworm.com/index.php?rid=3331983&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20193679%26dopt%3DAbstract This study showed that amlodipine prevents the reduction in bone density during the repeated dosing in SHR-sp. Amlodipine might exert its effect through a direct inhibition of osteoclast function and/or suppression of PTH secretion and subsequent inhibition of osteoclast activity. PMID: 20193679 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3331983 Fri, 26 Feb 2010 00:00:00 +0100 3331983 http://www.medworm.com/index.php?rid=3323131&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20188724%26dopt%3DAbstract In conclusion, present findings provide implication that the spinal anti-nociceptive mechanistic site of pregabalin is different from that of ziconotide, mexiletine, and duloxetine, and pregabalin could have a broader anti-nociceptive mechanism other than N-type calcium channel blockade. PMID: 20188724 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3323131 Wed, 24 Feb 2010 00:00:00 +0100 3323131 http://www.medworm.com/index.php?rid=3323130&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20188725%26dopt%3DAbstract Authors: Nasehi M, Piri M, Nouri M, Farzin D, Nayer-Nouri T, Zarrindast MR Ingestion of harmane and other alkaloids derived from plant Peganum harmala has been shown to elicit profound behavioral and toxic effects in humans, including hallucinations, excitation, feelings of elation, and euphoria. These alkaloids in the high doses can cause a toxic syndrome characterized by tremors and convulsions. Harmane has also been shown to act on a variety of receptor systems in the mammalian brain, including those for serotonin, dopamine and benzodiazepines. In animals, it has been reported to affect short and long term memory. In the present study, effects of dopamine D(1) and D(2) receptor antagonists on the harmane (HA)-induced amnesia and exploratory behaviors were examined in mice. One-trial... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3323130 Wed, 24 Feb 2010 00:00:00 +0100 3323130 http://www.medworm.com/index.php?rid=3323129&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20188726%26dopt%3DAbstract Authors: Kalonia H, Kumar P, Kumar A Objective of the present study was to explore the possible role of oxidative stress in the malonic acid - induced behavioral, biochemical and mitochondrial alterations in rats. In the present study, unilateral single injections of malonic acid at different doses (1.5, 3 and 6micromol) were made into the ipsilateral striatum in rats. Behavioral parameters were accessed on 1st, 7th and 14th day post malonic acid administration. Oxidative stress parameters and mitochondrial enzyme functions were assessed on day 14th after behavioral observations. Ipsilateral striatal malonic acid (3 and 6micromol) administration significantly reduced body weight, locomotor activity, motor coordination and caused oxidative damage (Lipid peroxidation, nitrite, superoxide... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3323129 Wed, 24 Feb 2010 00:00:00 +0100 3323129 http://www.medworm.com/index.php?rid=3323128&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20188727%26dopt%3DAbstract Authors: Aziz Q, Thomas A, Khambra T, Tinker A The biguanides, phenformin and metformin, are used in the treatment of type II diabetes mellitus, as well as being routinely used in studies investigating AMPK activity. We used the patch-clamp technique and rubidium flux assays to determine the role of these drugs in ATP sensitive K(+) channel (K(ATP)) regulation in cell lines expressing the cloned components of K(ATP) and the current natively expressed in vascular smooth muscle cells (VSMCs). Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1). However it does not inhibit the current potentially present in... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3323128 Wed, 24 Feb 2010 00:00:00 +0100 3323128 http://www.medworm.com/index.php?rid=3312489&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184872%26dopt%3DAbstract Authors: Vicente MI, Costa PF, Lima PA Galantamine, one of the major drugs used in Alzheimer's disease therapy, is a relatively weak acetylcholinesterase inhibitor and an allosteric potentiating ligand of nicotinic acetylcholine receptors. However, a role in the control of excitability has also been attributed to galantamine via modulation of K(+) currents in central neurones. To further investigate the effect of galantamine on voltage-activated K(+) currents, we performed whole-cell voltage-clamp recordings in differentiated neuroblastoma N1E-115 cells and in dissociated rat CA1 neurones. In both cell models, one can identify two main voltage-activated K(+) current components: a relatively fast inactivating component (Ifast; time constant approximately hundred milliseconds) and a slow... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312489 Mon, 22 Feb 2010 00:00:00 +0100 3312489 http://www.medworm.com/index.php?rid=3312488&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184873%26dopt%3DAbstract Authors: Maicas N, Ferrándiz ML, Devesa I, Motterlini R, Koenders MI, van den Berg WB, Alcaraz MJ Carbon monoxide-releasing molecules can counteract inflammatory responses. The aim of this study was to investigate whether tricarbonylchloro(glycinate)ruthenium (II) (CORM-3) is able to control the effector phase of experimental arthritis. Arthritis was induced in C57Black-6 mice by an intraperitoneal injection of serum from arthritic K/BxN mice. CORM-3 was administered intraperitoneally at 10mg/kg/day (5mg/kg twice a day) from days 0 to 10 and animals were sacrificed on day 11. Serum levels of osteocalcin and prostanoids were measured by enzyme-linked immunosorbent assay and radioimmunoassay. Gene expression was determined by real time PCR. Histological analysis was performed and pr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312488 Mon, 22 Feb 2010 00:00:00 +0100 3312488 http://www.medworm.com/index.php?rid=3312487&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184874%26dopt%3DAbstract This study was designed to examine if organ culture of rat bronchial segments induces airway hyperresponsiveness to bradykinin and if inhibition of IKK can abrogate the airway hyperresponsiveness to bradykinin via suppressing the expression of bradykinin B(1) and B(2) receptors. Rat bronchi were isolated and cut into ring segments. The segments were then organ cultured in the presence or absence of IKK inhibitors, BMS-345541 or TPCA-1. des-Arg(9)-bradykinin (B(1) receptor agonist) and bradykinin (B(2) receptor agonist) induced contractions of the segments as monitored by a sensitive organ bath system. The expression of bradykinin B(1) and B(2) receptors, inflammatory mediators and phosphorylated IKK were studied by a real-time PCR and/or by immunohistochemsity using confocal microscopy. Or... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312487 Mon, 22 Feb 2010 00:00:00 +0100 3312487 http://www.medworm.com/index.php?rid=3312486&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184875%26dopt%3DAbstract In conclusion, our results show that anti-IL-6 receptor antibody significantly (but only partially) suppressed the T cell receptor signalling-induced activation of CD4 T cells and also suggest that it achieved this partial suppression by the partial inhibition of IL-2 production and the induction of regulatory T cells. In stark contrast, anti-TNFalpha antibody had no impact on T cell activation. Extrapolating these results to the clinical treatment of rheumatoid arthritis, they suggest that IL-6 blockade inhibits T cell activation, whereas TNFalpha blockade does not. PMID: 20184875 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312486 Mon, 22 Feb 2010 00:00:00 +0100 3312486 http://www.medworm.com/index.php?rid=3312485&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184876%26dopt%3DAbstract Authors: Zarifkar A, Choopani S, Ghasemi R, Naghdi N, Maghsoudi AH, Maghsoudi N, Rastegar K, Moosavi M Neuroinflammation is associated with a number of neurodegenerative diseases. It is known that lipopolysaccharide (LPS) treatment induces neuroinflammation and memory deterioration. Agmatine, the metabolite of arginine by arginine decarboxylase, is suggested to be a neuroprotective agent. The aim of this study was to explore if agmatine can prevent LPS-induced spatial memory impairment and hippocampal apoptosis. Adult male Wistar rats (200-250g) were trained in water maze for 4days (3days in hidden platform and the last day in visible platform task). Saline, LPS (250microg/kg/ip) or (and) agmatine (5 or 10mg/kg) were administered 4 hours before every training session. LPS treatment imp... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312485 Mon, 22 Feb 2010 00:00:00 +0100 3312485 http://www.medworm.com/index.php?rid=3312484&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184877%26dopt%3DAbstract Authors: Abin-Carriquiry JA, Urbanavicius J, Scorza C, Rebolledo-Fuentes M, Wonnacott S, Cassels BK, Dajas F Nicotinic acetylcholine receptors influence striatal dopaminergic activity and its outcome on motor behavior. For these reasons, nicotinic receptors have been considered as therapeutically relevant targets for Parkinson's disease, in which a dramatic loss of dopamine affects motor functions. The aim of the present work was to compare the effects on locomotor activity induced by the nicotinic agonist cytisine and two brominated derivatives, 5- and 3-bromocytisine (5-BrCy and 3-BrCy) using nicotine for comparison. After acute systemic administration of the agonists only 3-BrCy induced an increase in locomotor activity. To study the mechanism of action involved in this increase we ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312484 Mon, 22 Feb 2010 00:00:00 +0100 3312484 http://www.medworm.com/index.php?rid=3312483&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184878%26dopt%3DAbstract This study also suggests that neuronal and astrocytic plasma membrane and/or mitochondrial K(ATP) channels may be a novel target that deserves attention for antipsychotic drug development. Future research using other sensitive tests is needed to confirm this property of iptakalim. PMID: 20184878 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312483 Mon, 22 Feb 2010 00:00:00 +0100 3312483 http://www.medworm.com/index.php?rid=3312482&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20184879%26dopt%3DAbstract Authors: Geng J, Peng W, Hou Y, Fan H, Li S Panax notoginseng saponins have recently been reported to suppress liver fibrosis. Since ginsenoside-Rg1 is the most abundant component of Panax notoginseng saponins, we investigated the effect of ginsenoside-Rg1 on experimental liver fibrosis in rats. Histological analysis revealed that ginsenoside-Rg1 significantly improved the extent of liver fibrosis in rats induced by thioacetamide. Ginsenoside-Rg1 markedly suppressed the serum levels of fibrotic markers and hepatic hydroxyproline content in rats treated with thioacetamide. Ginsenoside-Rg1 also reduced the serum levels of alanine transaminase, aspartate transaminase and alkaline phosphatase. Finally, ginsenoside-Rg1 attenuated the levels of thiobarbituric acid reactive substances in live... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312482 Mon, 22 Feb 2010 00:00:00 +0100 3312482 http://www.medworm.com/index.php?rid=3312493&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20176011%26dopt%3DAbstract Authors: Shakirova Y, Mori M, Ekman M, Erjefält J, Uvelius B, Swärd K Voiding is mediated by muscarinic receptors in urinary bladder smooth muscle cells. Lipid rafts and caveolae are cholesterol enriched membrane domains that modulate the activity of G protein-coupled receptors and second messenger systems. Conflicting findings regarding sensitivity of muscarinic signalling to cholesterol desorption, which perturbs lipid rafts and caveolae, have been reported, and no study has used human urinary bladder. Here, the dependence of human bladder muscarinic receptor signalling on plasma membrane cholesterol was examined. Nerve-mediated contraction, elicited by electrical field stimulation of human bladder strips, was impaired by desorption of cholesterol using methyl-beta-cyclodex... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312493 Fri, 19 Feb 2010 00:00:00 +0100 3312493 http://www.medworm.com/index.php?rid=3312492&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20176012%26dopt%3DAbstract Authors: Brändén L, Fredriksson A, Harring E, Jensen J, Lehmann A While patients with symptoms of gastroesophageal reflux disease generally respond well to proton pump inhibitors, 20-30% continue to experience troublesome symptoms. In such cases, agents that target transient lower esophageal sphincter (LES) relaxation may be useful as add-on therapy to proton pump inhibitors. The GABA(B) receptor agonist baclofen inhibits transient LES relaxation but it is not an ideal agent due to central nervous system activity. Lesogaberan (AZD3355) is a peripherally acting GABA(B) receptor agonist with limited central nervous system activity that inhibits transient LES relaxation in dogs. In the present study, the comparative effects of lesogaberan (7micromol/kg) and baclofen (2.8mumol/kg... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312492 Fri, 19 Feb 2010 00:00:00 +0100 3312492 http://www.medworm.com/index.php?rid=3312491&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20176013%26dopt%3DAbstract Authors: Sugimoto Y, Furutani S, Nishimura K, Itoh A, Tanahashi T, Nakajima H, Oshiro H, Sun S, Yamada J The effects of neferine, an alkaloid of Nelumbo Garther embryos, on immobility in the forced swimming test, which is used to evaluate antidepressants, were investigated in mice. The administration of neferine from 25 to 100mg/kgi.p. elicited anti-immobility effects in mice. The molecular dose effects of neferine in the forced swimming test were almost equal to those of the typical antidepressants maprotiline and imipramine. The involvement of the 5-HT receptor subtypes was also studied using 5-HT receptor antagonists. Anti-immobility effects of neferine are antagonized by the serotonin(1A) (5-HT(1A)) receptor antagonist, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N- (2-pyridinyl... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312491 Fri, 19 Feb 2010 00:00:00 +0100 3312491 http://www.medworm.com/index.php?rid=3312490&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20176014%26dopt%3DAbstract Authors: Mishra AC, Mohanty B Body weight gain, sexual/reproductive dysfunction and hematological abnormalities are serious consequences of atypical antipsychotics treatment. No attempts however have been made preclinically to elucidate the adverse hematological impacts. Presently, effects of lactational exposure of olanzapine (4, 8 and 10mg/kg) and risperidone (1 and 2mg/kg) on hematology as well as lymphoid organ histopathology of mice neonates were investigated. Both olanzapine and risperidone transfers through milk and make the neonates susceptible to their adverse side effects. Corticosterone elevation tendency of both the drugs further enhance the susceptibility for immune dysfunction. Analysis of total and differential leukocytes counts revealed neutropenia with all the doses of... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3312490 Fri, 19 Feb 2010 00:00:00 +0100 3312490 http://www.medworm.com/index.php?rid=3298727&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20171207%26dopt%3DAbstract Authors: Faron-Górecka A, Gąska M, Kuśmider M, Frankowska M, Adamczyk P, Filip M, Dziedzicka-Wasylewska M The level of mRNA encoding calcyon (measured by in situ hybridization), one of the dopamine receptor interacting proteins, has been examined in the rat brain in the established animal model used to study the mechanisms of cocaine addiction (cocaine self-administration involving a yoked procedure). Two weeks of cocaine self-administration (maintenance) did not affect the level of calcyon mRNA, regardless of the way cocaine was delivered, except for tuberculum olfactorium, where calcyon mRNA was increased after cocaine treatment. In the reinstatement phase of the experiment cocaine alone induced an increase in the calcyon mRNA expression in most of the brain region s... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3298727 Wed, 17 Feb 2010 00:00:00 +0100 3298727 http://www.medworm.com/index.php?rid=3298726&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20171208%26dopt%3DAbstract In conclusion, results indicate that AM404 inhibits directly the function of L-type voltage-dependent Ca(2+) channels in mammalian skeletal muscles. PMID: 20171208 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3298726 Wed, 17 Feb 2010 00:00:00 +0100 3298726 http://www.medworm.com/index.php?rid=3298728&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20170649%26dopt%3DAbstract In conclusion, D24, other isocyanine congeners and chemically-related adrenergic agents inhibit OCT-mediated [(3)H]MPP(+) transport, and all drugs display significant activity at alpha(1)- and alpha(2)- adrenoceptor subtypes, expanding previous reports of promiscuity between pharmacophores recognising alpha- adrenoceptors and OCTs. PMID: 20170649 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3298728 Tue, 16 Feb 2010 00:00:00 +0100 3298728 http://www.medworm.com/index.php?rid=3292156&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20167215%26dopt%3DAbstract Authors: Peng HJ, Dai DZ, Ji H, Dai Y Stress may affect gap junction connexin 43 and matrix metalloproteinase-2/9 (MMP-2/9) in cardiac fibroblasts, potentially contributing to worsening cardiac function and arrhythmias. Cardiac fibroblasts isolated from neonatal rat were incubated with isoproterenol at 3x10(-7)M to mimic stress and were treated with either PD156707 or IRL-1038 (selective antagonists for endothelin A and B receptor respectively) and CPU0213 (a dual endothelin A/B receptor antagonist) at 1x10(-8)M, 3x10(-8)M or 1x10(-7)M. RT-PCR and Western blotting were conducted. Upregulation of the two endothelin receptors, MMP-2/9 and NADPH oxidase subunits (p22phox and p47phox), and downregulation of connexin 43 in cardiac fibroblasts were found in the presence of isoproterenol and ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3292156 Mon, 15 Feb 2010 00:00:00 +0100 3292156 http://www.medworm.com/index.php?rid=3288481&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20159010%26dopt%3DAbstract In this study, the inhibitory effects of inflexin, a putative antiinflammatory agent isolated from Isodon excisus (Max.) Kudo (Labiateae), on the production of proinflammatory mediators was investigated in the lipopolysaccharide (LPS)-stimulated microglia. Inflexin significantly inhibited the release of nitric oxide (NO). Consistently, both the mRNA and the protein levels for the inducible NO synthase were decreased by inflexin in a concentration-dependent manner. Inflexin also inhibited the expression of cyclooxygenase (COX)-2, but not the COX-1 and effectively reduced the LPS-induced expression of proinflammatory cytokines in a dose-dependent manner. Furthermore, inflexin inhibited the degradation of IkappaB-alpha and the activation of NF-kappaB, p65 and Akt, while the MAPKs signal pathw... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288481 Sat, 13 Feb 2010 00:00:00 +0100 3288481 http://www.medworm.com/index.php?rid=3288484&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20156432%26dopt%3DAbstract In this study, we examined the role of adipocyte-generated angiotensin II in PVAT-mediated potentiation of contraction to nerve stimulation. In rat mesenteric PVAT, the presence of angiotesinogen and angiotensin I-converting enzyme (ACE) mRNA was confirmed by RT-PCR. Immunohistochemical staining showed the presence of angiotensin II in mesenteric PVAT. In rat mesenteric arteries, treatment of the vessels with an ACE inhibitor (enalaprilat) or angiotensin II type 1 receptor antagonist (candesartan) reduced PVAT-mediated potentiation of EFS-induced contraction. Exogenously applied angiotensin II enhanced EFS-induced contraction in arteries without PVAT, but not in the arteries with intact PVAT. Chronic treatment with an ACE inhibitor quinapril (14 days) lowered blood pressure and alleviated ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288484 Fri, 12 Feb 2010 00:00:00 +0100 3288484 http://www.medworm.com/index.php?rid=3288485&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20153745%26dopt%3DAbstract Authors: Prins J, Denys DA, Westphal KG, Korte-Bouws GA, Quinton MS, Schreiber R, Groenink L, Olivier B, Korte SM The first line of antidepressant treatment nowadays are selective serotonin reuptake inhibitors. Although they are relatively safe to use, selective serotonin reuptake inhibitors (SSRIs) can induce severe side effects. New promising antidepressants may be the triple monoamine reuptake inhibitors, which not only enhance serotonin and norepinephrine neurotransmission, but also increase brain dopamine levels. Recently it has been shown that one of the triple reuptake inhibitors, DOV 216,303 has antidepressant-like effects in the olfactory bulbectomy (OBX) model of depression, but the alterations in monoaminergic neurotransmission in these animals are still unknown. In the pres... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288485 Thu, 11 Feb 2010 00:00:00 +0100 3288485 http://www.medworm.com/index.php?rid=3288490&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20153312%26dopt%3DAbstract Authors: Campanholle G, Landgraf RG, Borducchi E, Semedo P, Wang PH, Amano MT, Russo M, Pacheco-Silva A, Jancar S, Camara NO Lipopolysaccharides from gram-negative bacteria are amongst the most common causative agents of acute lung injury, which is characterized by an inflammatory response, with cellular infiltration and the release of mediators/cytokines. There is evidence that bradykinin plays a role in lung inflammation in asthma but in other types of lung inflammation its role is less clear. In the present study we evaluated the role of the bradykinin B(1) receptor in acute lung injury caused by lipopolysaccharide inhalation and the mechanisms behind bradykinin actions participating in the inflammatory response. We found that in C57Bl/6 mice, the bradykinin B(1) receptor expression... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288490 Wed, 10 Feb 2010 00:00:00 +0100 3288490 http://www.medworm.com/index.php?rid=3288489&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20153313%26dopt%3DAbstract Authors: Sedaghati M, Vousooghi N, Goodarzi A, Yaghmaei P, Mokri A, Zarrindast MR Glutamate is critically involved in opioid addiction. It has been suggested that neurotransmitter receptors expression in peripheral blood lymphocytes may reflect brain status. In the present study, using Real-time PCR, the mRNA expression of NR2D and NR3B subunits of NMDA glutamate receptor has been investigated in peripheral blood lymphocytes of four groups each comprising of 25 male individuals: opioid addicts, methadone maintained patients, long-term abstinent former opioid addicts, and non-addicted control subjects. We found that NR2D subunit mRNA expression was not changed in all three test groups in comparison to control subjects. However, the NR3B mRNA expression was significantly up-regulated by ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288489 Wed, 10 Feb 2010 00:00:00 +0100 3288489 http://www.medworm.com/index.php?rid=3288488&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20153314%26dopt%3DAbstract Authors: Schindler CW, Panlilio LV, Gilman JP, Justinova Z, Vemuri K, Makriyannis A, Goldberg SR Cannabinoid-receptor antagonists have shown some promise as treatments capable of reducing abuse and relapse to a number of abused drugs. In rodents, such effects have been observed with methamphetamine self-administration. However, the effects of cannabinoid receptor antagonists on methamphetamine self-administration and relapse have not been studied in primates. In the present study, rhesus monkeys were trained to respond on a three-component operant schedule. During the first 5-min component, fixed-ratio responses were reinforced by food, during the second 90- or 180-min component fixed-ratio responses were reinforced by i.v. methamphetamine. The third component was identical to the firs... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288488 Wed, 10 Feb 2010 00:00:00 +0100 3288488 http://www.medworm.com/index.php?rid=3288487&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20153315%26dopt%3DAbstract In this study, we established the treatment paradigms for an in vitro model of tolerance to oxidative injury in primary astrocytic cultures and further examined the roles for the HIF-1 signalling cascade. Isolated murine astrocytes were preconditioned with sub-toxic concentrations of HIF-1 inducers and subsequently exposed to a H(2)O(2) insult, where changes in cell viability and protein expression were determined. Preconditioning with non-damaging concentrations of desferrioxamine (DFO) and ethyl-3,4-dihydroxybenzoate (EDHB) significantly improved cellular viability after H(2)O(2) injury treatment. Time course studies revealed that DFO and EDHB treatments alone induced sequential activation of HIF-1 signal transduction where nuclear HIF-1alpha protein accumulation was detected as early as... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288487 Wed, 10 Feb 2010 00:00:00 +0100 3288487 http://www.medworm.com/index.php?rid=3288486&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20153316%26dopt%3DAbstract Authors: Bianchi BR, El Kouhen R, Chen J, Puttfarcken PS A-778317 (1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea) is a potent antagonist of human and rat transient receptor potential vanilloid-1 (TRPV1) receptors. We have previously reported that [(3)H]A-778317 is an excellent radioligand to study the recombinant human TRPV1 receptor in a heterologous expression system. These studies were extended to determine the feasibility of using [(3)H]A-778317 to label native TRPV1 channels in rat tissues. Saturable high-affinity binding of [(3)H]A-778317 was detected in membrane preparations of rat dorsal root ganglia (DRG) and spinal cord that was inhibited by TRPV1 receptor agonists and antagonists. [(3)H]A-778317 labeled a single class of high-affinity binding sites in both rat DRG ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288486 Wed, 10 Feb 2010 00:00:00 +0100 3288486 http://www.medworm.com/index.php?rid=3288492&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20152830%26dopt%3DAbstract This article aims to review the potential pleiotropic effects of the drug mainly on inflammation markers, lipoprotein subfractions and endothelial function. PMID: 20152830 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288492 Tue, 09 Feb 2010 00:00:00 +0100 3288492 http://www.medworm.com/index.php?rid=3288491&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20152831%26dopt%3DAbstract Authors: Guabiraba R, Campanha AL, Souza AL, Santiago HC, Lugnier C, Alvarez-Leite J, Lemos VS, Teixeira MM Reactive oxygen species, cytokines and chemokines produced at inflammatory sites are pivotal events in the progression of many diseases. Flavonoids are well-known for their antioxidant and anti-inflammatory activities. Here, we investigated the effects of the flavonoid dioclein on the production of mediators of inflammation in vitro and possible underlying mechanisms. Murine macrophages were pretreated with dioclein, rolipram, a PDE4 (cyclic nucleotide phosphosdiesterase type 4) inhibitor, or butylated hydroxytoluene (BHT), an antioxidant, and then activated with LPS or LPS/IFN-gamma. The concentration of TNF-alpha, IL-6, CXCL1/KC, CCL2/JE, and nitric oxide (NO) was determined on... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3288491 Tue, 09 Feb 2010 00:00:00 +0100 3288491 http://www.medworm.com/index.php?rid=3270283&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20149790%26dopt%3DAbstract Authors: Patel NJ, Chen MJ, Russo-Neustadt AA Nitric oxide (NO), physical exercise and/or antidepressant drugs, through the increased release of norepinephrine and brain-derived neurotrophic factor (BDNF), have been shown to exert profound protective, pro-survival effects on neurons otherwise compromised by injury, disease, prolonged stress, and subsequent depression in vivo. We sought, therefore, to evaluate such survival and neuroprotection in hippocampal neurons in culture, which, in an analogous model of in vivo cellular stress, was deprived of several vital nutrients. We assessed pro-survival outcomes following the application of norepinephrine or the noradrenergic partial agonist, clonidine, a general nitric oxide synthase inhibitor and NO donor, using a cell survival assay and q... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3270283 Mon, 08 Feb 2010 00:00:00 +0100 3270283 http://www.medworm.com/index.php?rid=3257595&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20138862%26dopt%3DAbstract Authors: Stadel R, Carpenter AB, Nalwalk JW, de Esch IJ, Janssen E, Hough LB [(3)H]Cimetidine, a radiolabeled histamine H(2) receptor antagonist, binds with high affinity to an unknown hemoprotein in the brain which is not the histamine H(2) receptor. Improgan, a close chemical congener of cimetidine, is a highly effective pain-relieving drug following CNS administration, yet its mechanism of action remains unknown. To test the hypothesis that the [(3)H]cimetidine-binding site is the improgan antinociceptive target, improgan, cimetidine, and 8 other chemical congeners were studied as potential inhibitors of [(3)H]cimetidine binding in membrane fractions from the rat brain. All compounds produced a concentration-dependent inhibition of [(3)H]cimetidine binding over a 500-fold range of p... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3257595 Thu, 04 Feb 2010 00:00:00 +0100 3257595 http://www.medworm.com/index.php?rid=3247302&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20132809%26dopt%3DAbstract Authors: Sánchez-Fidalgo S, Cárdeno A, Villegas I, Talero E, la Lastra CA Ulcerative colitis is a nonspecific inflammatory disorder characterized by oxidative and nitrosative stress, leucocyte infiltration and upregulation of inflammatory mediators. Resveratrol is a polyphenolic compound found in grapes and wine, with multiple pharmacological actions, mainly anti-inflammatory, antioxidant, antitumour and immunomodulatory activities. The aim of this study was to investigate the effect of dietary resveratrol on chronic dextran sulfate sodium (DSS)-induced colitis. Six-week-old mice were randomized into two dietary groups: one standard diet and other enriched with resveratrol at 20mg/Kg of diet. After 30days, mice were exposed to 3% DSS for 5days developing acute colitis that pr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3247302 Mon, 01 Feb 2010 00:00:00 +0100 3247302 http://www.medworm.com/index.php?rid=3247301&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20132810%26dopt%3DAbstract Authors: Goto M, Kadoshima-Yamaoka K, Murakawa M, Yoshioka R, Tanaka Y, Inoue H, Murafuji H, Kanki S, Hayashi Y, Nagahira K, Ogata A, Nakatsuka T, Fukuda Y Excessive proliferation of epidermal keratinocytes is a typical aspect of chronic skin diseases such as psoriasis. In the present study, effect of phosphodiesterase 7A (PDE7A) inhibitor ASB16165 on proliferation of keratinocytes was investigated to examine the role of PDE7A in keratinocyte proliferation and the possible therapeutic relevance of PDE7A inhibition in psoriasis. Topical application of ASB16165 inhibited the increase of thickness of skin as well as epidermis in a skin inflammation model induced by repeated painting of 12-O-tetradecanoylphorbol-13-acetate (TPA) in a concentration-dependent manner. The ASB16165 treatment a... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3247301 Mon, 01 Feb 2010 00:00:00 +0100 3247301 http://www.medworm.com/index.php?rid=3247300&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20132811%26dopt%3DAbstract Authors: Yang LZ, Tovote P, Rayner M, Kockskämper J, Pieske B, Spiess J Corticotropin-releasing factor (CRF), a 41 amino acid peptide, was discovered as a key signal in mediating neuroendocrine, autonomic, and behavioral responses to stress. It was revealed later that there exist additional CRF like peptides, termed urocortins. The CRF receptor subtype 1 (CRF1 receptor) is predominant in the brain whereas subtype 2 (CRF2 receptor) is highly expressed in brain and heart. Both centrally and peripherally administered CRF and urocortins produce significant hemodynamic effects via activation of CRF receptors in brain and heart. CRF and urocortins are important neural and cardioactive hormones, and are potentially useful therapy for heart failure. PMID: 20132811 [PubMed - as supplie... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3247300 Mon, 01 Feb 2010 00:00:00 +0100 3247300 http://www.medworm.com/index.php?rid=3247299&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20132812%26dopt%3DAbstract In conclusion, the present study shows that oral iAP administration has beneficial effects in situations of severe intestinal epithelial damage, whereas in moderate inflammation endogenous iAP may be sufficient to counteract disease-aggravating effects of LPS. An approach including iAP treatment holds a therapeutic promise in case of severe inflammatory bowel disease. PMID: 20132812 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3247299 Mon, 01 Feb 2010 00:00:00 +0100 3247299 http://www.medworm.com/index.php?rid=3247298&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20132813%26dopt%3DAbstract Authors: Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst J, Gibbs A, Kahl J, Kessler L, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Wang Z, Larson CJ The tumor necrosis factor-alpha (TNF-alpha) cytokine, secreted by activated monocytes/macrophages and T lymphocytes, is implicated in several diseases, including rheumatoid arthritis, chronic obstructive pulmonary disease, inflammatory bowel disease, and osteoporosis. Monocyte/macrophage production of TNF-alpha is largely driven by p38alpha mitogen activated protein kinase (MAP kinase), an intracellular soluble serine-threonine kinase. p38alpha MAP kinase is activated by growth factors, cellular stresses, and cytokines such as TNF-alpha and interleukin-l (IL-I). The pri... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3247298 Mon, 01 Feb 2010 00:00:00 +0100 3247298 http://www.medworm.com/index.php?rid=3240201&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20122922%26dopt%3DAbstract Authors: Elaković I, Vasiljević D, Adžić M, Dorđević A, Dorđević J, Radojčić M, Matić G Gender-related differences in the expression and functional properties of the hepatic glucocorticoid receptor were studied before and after antidepressant fluoxetine administration to both unstressed and rats exposed to a chronic social isolation stress. Some of the receptor's functional properties, including hormone-binding capacity (B(max)), hormone-binding potency (B(max)/K(D) ratio) and the DNA-binding ability, were found to be sexually dimorphic. Fluoxetine treatment (5mg/kg body mass, 21day, intraperitoneally) induced a decrease in B(max) and in the amount of Hsp70 co-immunoprecipitated with the glucocorticoid receptor only in m... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240201 Sat, 30 Jan 2010 00:00:00 +0100 3240201 http://www.medworm.com/index.php?rid=3240199&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20123095%26dopt%3DAbstract In conclusion, we have found that L-carnitine and captopril have a similar antioxidant effect in the hearts of hypertensive rats. The molecular regulation of antioxidant enzymes through an inhibition of the renin-angiotensin system and a modulation of the NF-kB/IkB system seems to be responsible for this antioxidant effect. PMID: 20123095 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240199 Sat, 30 Jan 2010 00:00:00 +0100 3240199 http://www.medworm.com/index.php?rid=3240198&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20123096%26dopt%3DAbstract Authors: Yeh CH, Chen ZC, Hsu CC, Lin MT, Chen CC The present study was attempted to evaluate the therapeutic effects of activated protein C and/or hyperbaric oxygen in an animal model of heatstroke. Sixty-eight mins heat stress (43 degrees C) initiated, the anesthetized rats were randomized to several groups and administered: 1) no resuscitation (vehicle solution plus normabaric air, 2) intravenous activated protein C (1mg in 1ml of normal saline per kg of body weight), 3) hyperbaric oxygen (100% oxygen at 202kpa for 17min), and 4) intravenous activated protein C plus hyperbaric oxygen. Another group of rats exposed to room temperature (26 degrees C) was used as normothermic controls. Blood sampling was 0min, 70min, and 85min after heat stress initiated. When the vehicle-treated rats ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240198 Sat, 30 Jan 2010 00:00:00 +0100 3240198 http://www.medworm.com/index.php?rid=3240197&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20123097%26dopt%3DAbstract Authors: Bach-Rojecky L, Salković-Petrišić M, Lacković Z We investigated antinociceptive activity of botulinum toxin type A (BTX-A) in a model of diabetic neuropathic pain in rats. Male Wistar rats were made diabetic by a single intraperitoneal injection of streptozotocin (80mg/kg). Sensitivity to mechanical and thermal stimuli was measured with the paw-pressure and hot-plate test, respectively. The formalin test was used to measure sensitivity to chemical stimuli. Diabetic animals with pain thresholds lower for at least 25% compared to the non-diabetic group were considered neuropathic and were injected with BTX-A either subcutaneously (3, 5 and 7U/kg) or intrathecally (1U/kg). Mechanical and thermal sensitivity was measured at several time-points. After periph... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240197 Sat, 30 Jan 2010 00:00:00 +0100 3240197 http://www.medworm.com/index.php?rid=3240196&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20123098%26dopt%3DAbstract The objective of this study was to establish if aging impairs the response to an antidepressant by using an animal model. For this purpose, young and middle-aged male Wistar rats (of around 4 and 14months, respectively) were exposed to a chronic mild stress schedule for 3weeks. After this period, the animals that developed anhedonia, reflected as a reduction in sucrose solution (1%) intake, were treated with citalopram (10mg/kg/day) during 21days while still maintained under the chronic mild stress schedule. Non-stressed animals were included as controls. In young rats citalopram reversed the reduction in sucrose consumption induced by chronic mild stress after one week of treatment, while in middle-aged animals a similar reversion occured after three weeks. Citalopram did not importantly ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240196 Sat, 30 Jan 2010 00:00:00 +0100 3240196 http://www.medworm.com/index.php?rid=3240195&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20123099%26dopt%3DAbstract Authors: Li J, Xiao J, Liang D, Zhang H, Zhang G, Liu Y, Zhang Y, Liu Y, Yu Z, Yan B, Jiang B, Li F, Peng L, Zhou ZN, Chen YH Atrial fibrillation is the most common arrhythmia encountered in clinical practice. It can cause severe complications such as congestive heart failure and stroke. However, identification of prime targets for efficient therapeutic intervention remains a challenge. In vitro rabbit heart models of ischemia-, stretch-, and cholinergic agitation-induced atrial fibrillation were developed, and pharmacological interventions of mitochondrial translocator protein (TSPO) were adopted to explore the role of the mitochondrial protein in the aforementioned atrial fibrillations. Fura-2 AM and Mg(2+)-Fura-2 AM were used to monitor the alterations of intracellular Ca(2+) and AT... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240195 Sat, 30 Jan 2010 00:00:00 +0100 3240195 http://www.medworm.com/index.php?rid=3240203&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20122920%26dopt%3DAbstract Authors: Badole SL, Bodhankar SL The aim of the present investigation was to evaluate the antidiabetic activity of cycloart-23-ene-3beta, 25-diol (called as B2) isolated from stem bark of Pongamia pinnata in streptozotocin-nicotinamide induced diabetic mice. Diabetes was induced in mice by injecting streptozotocin (200mg/kg, i.p.) after 15min nicotinamide (110mg/kg, i.p.). The mice were divided into following groups; I- nondiabeteic, II- diabetic control, III- glybenclamide (10mg/kg, p.o.), IV- B2 (1mg/kg, p.o.) and V- B2 (3mg/kg, p.o., only for acute study). Serum glucose was determined periodically. Body weight, food and water intake were recorded daily. Oral glucose tolerance test was performed on day 28. Biochemical and enzyme antioxidant parameters were determined. Histology of pa... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240203 Fri, 29 Jan 2010 00:00:00 +0100 3240203 http://www.medworm.com/index.php?rid=3240202&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20122921%26dopt%3DAbstract Authors: Böer U, Noll C, Cierny I, Krause D, Hiemke C, Knepel W The transcription factor CREB regulates adaptive responses like memory consolidation, addiction, and synaptic refinement. Recently, chronic psychosocial stress as animal model of depression has been shown to stimulate CREB transcriptional activity in the brain; this stimulation was prevented by treatment with the antidepressant imipramine, which inhibits both noradrenaline and serotonin reuptake. However, it was unknown whether the selective inhibition of serotonin reuptake is sufficient for inhibition of stress-induced CREB activation, as it is for the clinical antidepressant effect. Therefore, the effect of two selective serotonin reuptake inhibitors (SSRIs), citalopram and fluoxetine, was examined in this study. Tr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240202 Fri, 29 Jan 2010 00:00:00 +0100 3240202 http://www.medworm.com/index.php?rid=3240200&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20122923%26dopt%3DAbstract This study applies new magnetic sensor-electromyographic technology for recording jaw movements in freely moving rats to analyse topographies of orofacial movement that occur in association with individual elements of behaviour under challenge with two dopamine D(1)-like receptor agonists, SKF 83822 ([R/S]-6-chloro-7, 8-dihydroxy-3-allyl-1-[3-methylphenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine) and SKF 83959([R/S]-3-methyl-6-chloro-7, 8-dihydroxy-1-[3-methyl-phenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine). Grooming of the snout/face involved primarily dominant-mouth opening jaw movements with small activation of digastric muscles; subsequent grooming of the flank/trunk was characterised by repetitive, uniform jaw movements with small activation of digastric and masseter muscles. In contrast, gr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3240200 Fri, 29 Jan 2010 00:00:00 +0100 3240200 http://www.medworm.com/index.php?rid=3208607&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20097192%26dopt%3DAbstract Authors: Gessner G, Macianskiene R, Starkus JG, Schönherr R, Heinemann SH Human ether à go-go related gene (hERG1) potassium channels underlie the repolarizing I(Kr) current in the heart. Since they are targets of various drugs with cardiac side effects we tested whether the amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015) blocks hERG1 channels like its parent compound. Using patch-clamp and two-electrode voltage-clamp techniques we found that KB130015 blocks native and recombinant hERG1 channels at high voltages, but it activates them at low voltages. The activating effect has an apparent EC(50) value of 12microM and is brought about by an about 4-fold acceleration of activation kinetics and a shift in voltage-dependent activation by ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208607 Thu, 21 Jan 2010 00:00:00 +0100 3208607 http://www.medworm.com/index.php?rid=3208605&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20097193%26dopt%3DAbstract Authors: Lee YC, Lin HH, Hsu CH, Wang CJ, Chiang TA, Chen JH Lung cancer is the leading cause of death among cancers worldwide and non-small cell lung cancer (NSCLC) comprises more than 80% of lung cancer cases. Treatment options for patients with advanced NSCLC have evolved in the last decade with the advent of novel biological agents. Andrographolide, a diterpenoid lactone isolated from a traditional herbal medicine Andrographis paniculata, is known to have the potential to be developed as a chemotherapeutic agent. In order to understand the anti-cancer properties of andrographolide, we examined its effect on migration and invasion in human NSCLC A549 cells. The results of wound-healing assay and in vitro transwell assay revealed andrographolide inhibited dose-dependently the migrati... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208605 Thu, 21 Jan 2010 00:00:00 +0100 3208605 http://www.medworm.com/index.php?rid=3208602&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20097194%26dopt%3DAbstract Authors: Miyashitaa Y, Furukawa T, Kamegaya E, Yoshii M, Nukada T Amlodipine, a dihydropyridine derivative, has been shown to block not only L-type but also N type Ca(2+) channels. Aiming to understand the mechanism underlying such a selective blockade by amlodipine, the interaction of amlodipine with N-type channels was investigated using the Xenopus oocyte expression system together with the two-microelectrode voltage-clamp technique and the binding assay for [(3)H]amlodipine. When expressed as the alpha1Balpha2/delta1beta1a combination, the N-type channel formed a high affinity binding site for [(3)H]amlodipine (K(d), 3.08nM) and was profoundly blocked by amlodipine (IC(50), 2.7muM at -60mV). By contrast, R type alpha1Ealpha2/delta1beta1a channels did not possess a high affinity bin... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208602 Thu, 21 Jan 2010 00:00:00 +0100 3208602 http://www.medworm.com/index.php?rid=3208608&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20096684%26dopt%3DAbstract Authors: Noguchi K, Hamadate N, Matsuzaki T, Sakanashi M, Nakasone J, Sakanashi M, Tsutsui M, Sakanashi M To investigate the role of tetrahydrobiopterin (BH4), an essential cofactor of nitric oxide synthase, in endothelial function in a model of genetic hypertension, acetylcholine- and sodium nitroprusside (SNP)-induced vasodilator responses were examined in the absence and presence of BH4 in age-matched adult stroke-prone spontaneously hypertensive rats (SHRSP) and Wistar-Kyoto (WKY) rats. Acetylcholine-induced depressor responses attenuated significantly in SHRSP compared with those in WKY rats. Acetylcholine-induced relaxations in phenylephrine-precontracted aortic rings of SHRSP were also significantly impaired as compared to those of WKY rats, while SNP-induced relaxations were si... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208608 Wed, 20 Jan 2010 00:00:00 +0100 3208608 http://www.medworm.com/index.php?rid=3208613&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20096281%26dopt%3DAbstract Authors: Liu CQ, Wong SL, Leung FP, Tian XY, Lau CW, Lu L, Yao X, Chen ZY, Yao T, Huang Y Activation of the thromboxane prostanoid (TP) receptor produces potent vasoconstriction, which contributes to the increased vascular tone and blood pressure. The present study was designed to examine the hypothesis that stimulation of prostanoid TP receptors impairs endothelium-independent relaxations to cyclic AMP-elevating agents via increasing the activity of phosphodiesterases (PDEs). Rat carotid arteries without endothelium were isolated and suspended in myograph for the measurement of changes in isometric tension; the tissue content of cyclic AMP was assayed by enzyme immunoassay kit; and prostanoid TP receptor was detected in vascular wall by immunohistochemistry and Western blot. In phenyl... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208613 Tue, 19 Jan 2010 00:00:00 +0100 3208613 http://www.medworm.com/index.php?rid=3208612&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20096282%26dopt%3DAbstract Authors: Lee CS, Kim YJ, Jang ER, Myung SC, Kim W Carboplatin and Akt inhibitor have been shown to induce apoptosis in cancer cells. However, the combined effect of Akt inhibitor on the apoptotic effect of carboplatin in epithelial ovarian cancer cells remains uncertain. In the respect of the induction of cell death signaling pathways, we assessed the combined effect of Akt inhibitor on the carboplatin toxicity in the human epithelial ovarian carcinoma cell lines OVCAR-3 and SK-OV-3. Carboplatin and Akt inhibitor induced nuclear damage, decreased Bid and Bcl-2 protein levels, induced cytochrome c release, activated caspase-3 and increased tumor suppressor p53 levels. Carboplatin increased in Bax levels, whereas Akt inhibitor decreased Bax levels. Akt inhibitor enhanced the carbopatin-i... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208612 Tue, 19 Jan 2010 00:00:00 +0100 3208612 http://www.medworm.com/index.php?rid=3208611&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20096283%26dopt%3DAbstract Authors: Yip KH, Huang Y, Leung FP, Lau HY We have previously demonstrated that exogenous nitric oxide (NO) inhibited anti-IgE-mediated histamine release from human cultured mast cells. In the current study, we further investigated if syntheses of eicosanoids and cytokines were also suppressed by NO donors and evaluated if activation of soluble guanylyl cyclase (sGC) was an underlying mechanism. The effects of the NO donor diethylamine NONOate (DEA/NO) on IgE-dependent syntheses of eicosanoids (prostaglandin D(2) and cysteinyl leukotrienes) and cytokines (tumor necrosis factor-alpha and interleukin-8) from buffy coat derived human cultured mast cells were examined. The effects of sGC related agents on human mast cell activation were studied by measuring histamine release. DEA/NO (10(-7... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208611 Tue, 19 Jan 2010 00:00:00 +0100 3208611 http://www.medworm.com/index.php?rid=3208609&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20096284%26dopt%3DAbstract Authors: Okada A, Kato A, Kamei C We investigated the effects of histamine H(1) receptor antagonists in different 3 stages of spatial working memory in comparison with scopolamine. The effects of drugs were measured using an eight-arm radial maze with a delayed spatial win-shift task in rats. Drugs were injected 10min before the training phase (timing 1), immediately after the training phase (timing 2), or 10min before the test phase (timing 3). Intrahippocampal injection of pyrilamine and diphenhydramine resulted in significant effects on the number of correct choices and across-phase errors in all 3 timings. Scopolamine impaired the number of correct choices and across-phase errors in timing 1 and 3; however, no significant effect was observed in timing 2. These results indicate that... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3208609 Tue, 19 Jan 2010 00:00:00 +0100 3208609 http://www.medworm.com/index.php?rid=3189910&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20079350%26dopt%3DAbstract Authors: Sun H, Che QM, Zhao X, Pu XP Baicalein was a major bioactive flavonoid derived from Radix Scutellariae in Xiao-Chai-Hu-Tang which was commonly used to treat chronic hepatitis and liver fibrosis in China. The aim of this study was to assess whether chronic baicalein administration could prevent liver fibrosis induced by carbon tetrachloride (CCl(4)) in rats and investigate its possible protective mechanism. The antifibrotic effects of baicalein were assessed directly by hepatic histology and indirectly by measuring levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), hepatic hyaluronic acid, laminin and procollagen type III (PCIII) in serum, as well as hydroxyproline and matrix metalloproteinases (MMPs) in liver. In addition, we further investigated prote... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3189910 Thu, 14 Jan 2010 00:00:00 +0100 3189910 http://www.medworm.com/index.php?rid=3189912&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20079349%26dopt%3DAbstract Authors: Araiza-Saldaña CI, Rocha-González HI, Ambriz-Tututi M, Castañeda-Corral G, Caram-Salas NL, Hong E, Granados-Soto V The possible antiallodynic effect of phosphodiesterease 5 inhibitor sildenafil and nitric oxide donor glyceryl trinitrate as well as the changes in phosphodiesterease 5A2 mRNA expression in dorsal root ganglion and spinal cord of allodynic diabetic rats was assessed. Diabetes was induced by streptozotocin (50mg/kg, i.p.) in male Wistar rats. Streptozotocin injection produced hyperlglycemia, polydipsia, polyphagia and plolyuria as well as long-term tactile allodynia (12weeks) and a reduction of phosphodiesterase 5A2 mRNA expression in spinal cord of diabetic rats. Systemic administration of sildenafil (1.8 - 5.6mg/kg, i.p.) reduced tactile allodynia ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3189912 Tue, 12 Jan 2010 00:00:00 +0100 3189912 http://www.medworm.com/index.php?rid=3172935&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20067787%26dopt%3DAbstract In this report, NP-184 inhibited the viability of human umbilical vascular endothelial cells (HUVEC) in a concentration-dependent manner, and caused cell apoptosis as examined by cell-cycle analysis and Annexin V-staining with flow cytometry. NP-184 also concentration-dependently inhibited the HUVEC migration, tube formation on Matrigel, and rat aortic ring sprouting stimulated by VEGF. Regarding the intracellular signal transduction, NP-184 concentration-dependently interfered with the activation of AKT, ERK and the nuclear translocation of NFkappaB. In vivo study showed that NP-184 dose-dependently reduced angiogenesis in Matrigel plug assay. These results indicate that NP-184 is a potential candidate for developing the treatment of angiogenesis related-diseases. PMID: 20067787 [PubM... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3172935 Sat, 09 Jan 2010 00:00:00 +0100 3172935 http://www.medworm.com/index.php?rid=3166988&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20064502%26dopt%3DAbstract Authors: He W, Cheng Z, Fu G, Xu X, Lu Q, Guo L Hyperpolarization-activated cyclic-nucleotide-gated (HCN) channels have been suggested to play an important role in the control of membrane excitability and rhythmic neuronal activity. Our previous study showed that the selective HCN channels blocker, ZD7288 (4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino) pyrimidinium chloride) can block the induction of long-term potentiation (LTP) in perforant path-CA3 region in rat hippocampus in vivo. In the present study, we investigated the effect of ZD7288 on synaptic transmission and high frequency stimulation (HFS)-induced LTP in the Schaffer collateral-CA1 synapse of rat hippocampus in vivo, and examined the possible relations between activation of N-methyl-D-aspartate (NMDA) type of glu... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3166988 Fri, 08 Jan 2010 00:00:00 +0100 3166988 http://www.medworm.com/index.php?rid=3166987&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20064503%26dopt%3DAbstract Authors: Khadeer Ahamed MB, Krishna V, Dandin CJ Grewia tiliaefolia is widely used in traditional Indian medicines to cure jaundice, biliousness, dysentery and the diseases of blood. Bioassay-guided fractionation of methanolic extract of G. tiliaefolia bark has resulted in the isolation of D-erythro-2-hexenoic acid gamma-lactone (EHGL) and gulonic acid gamma-lactone (GAGL). Hepatoprotective activity of methanolic extract and the isolated constituents were evaluated against CCl(4)-induced hepatotoxicity in rats. The treatment with methanolic extract, EHGL and GAGL at oral dose of 100, 150 and 60mg/kg respectively with concomitant CCl(4) intraperitoneal injection (1ml/kg) significantly reduced the elevated plasma levels of aminotransferases, alkaline phosphatase and the incidence of live... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3166987 Fri, 08 Jan 2010 00:00:00 +0100 3166987 http://www.medworm.com/index.php?rid=3156821&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20056114%26dopt%3DAbstract Authors: Joseph A, Kumar TP, Nandhu MS, Paulose CS Glucose homeostasis in humans is an important factor for the functioning of nervous system. A decrease in glucose content below a minimal level or hypoglycemia is dangerous for cells of the central and peripheral nerve system. In the present study we showed the effects of insulin induced hypoglycaemia and streptozotocin induced diabetes on the cerebellar glutamate receptor subunits and glutamate transporter. Cerebellar dysfunction is associated with seizure generation, motor deficits and memory impairment. We found an up regulation in NMDA receptor number and gene expression of N-methyl-D-aspartic acid (NMDA (R1)), NMDA(2B), metabotrophic glutamate 5 (mGlu(5)) glutamate receptor subunits in experimental rats. The glutamate content was ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3156821 Mon, 04 Jan 2010 00:00:00 +0100 3156821 http://www.medworm.com/index.php?rid=3156820&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20056115%26dopt%3DAbstract Authors: Kim SM, Lee SY, Cho JS, Son SM, Choi SS, Yun YP, Yoon DY, Oh KW, Han SB, Hong JT Ginsenoside Rg3 has been interested for using as a cancer preventive or therapeutic agent. Nuclear Factor-kappa (NF-kappaB) is constitutively activated in the prostate cancer, and gives cancer cells resistance to chemotherapeutic agents. To investigate whether Rg3 can suppress the activation of NF-kappaB, and thus increase susceptibility of prostate (LNCaP and PC-3, DU145) cells against chemotherapeutics, Prostate cancer cell growth as well as activation of NF-kappaB were examined. We found that the combination treatment of Rg3 (50muM) with conventional agent docetaxel (5nM) was more effective in the inhibition of prostate cancer cell growth and induction of apoptosis as well as G(0)/G(1) arrest a... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3156820 Mon, 04 Jan 2010 00:00:00 +0100 3156820 http://www.medworm.com/index.php?rid=3156819&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20056116%26dopt%3DAbstract Authors: Pushpavalli G, Kalaiarasi P, Veeramani C, Pugalendi KV Chrysin a natural, biologically active compound present in many plants and possesses potent antiinflammatory, anticancer and antioxidation properties. This work was designed to investigate the effect of chrysin, on the hepatoprotective efficacy in D-galactosamine-intoxication rats. D-galactosamine-induced toxicity was manifested by the elevation of serum hepatic markers enzyme activities (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and gamma glutamyl transpeptidase and lipid peroxidation process and by decreasing the antioxidant capacity of the plasma, erythrocyte and tissues. Treatment with chrysin (25, 50 and 100mg/kg body weight) decreased hepatic markers enzymes activities and lipid perox... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3156819 Mon, 04 Jan 2010 00:00:00 +0100 3156819 http://www.medworm.com/index.php?rid=3143244&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20045404%26dopt%3DAbstract In this study, we discovered a novel compound, Compound B, and characterized its biochemical and pharmacological properties. Compound B has a more appropriate profile for use as a pharmacological tool compared to Compound A. Chronic treatment with Compound B in model animals, diet-induced obesity (DIO) and KKAy mice, showed significant reduction in hepatic fatty acid composition, suggesting that it effectively inhibits ELOVL6 activity in the liver. However, no improvement in insulin resistance by ELOVL6 inhibition was found in these model animals. Further studies need to address the impact of ELOVL6 inhibition on pharmacological abnormalities in several model animals. This is the first report on pharmacology data from chronic studies using a selective ELOVL6 inhibitor. Compound B appears t... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143244 Wed, 30 Dec 2009 00:00:00 +0100 3143244 http://www.medworm.com/index.php?rid=3143243&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20045405%26dopt%3DAbstract This study tested the effects of lidocaine and procaine, alone and in combination with vecuronium and cisatracurium, on adult muscle-type nicotinic acetylcholine receptors. The adult mouse muscle-type nicotinic acetylcholine receptor was expressed in HEK293 cells and activated with 10microM acetylcholine. Currents were recorded using the whole-cell voltage clamp technique. Adult muscle-type nicotinic acetylcholine receptors were potently inhibited by all the tested compounds. Although the potencies of procaine and lidocaine were statistically significantly different at adult muscle-type nicotinic acetylcholine receptors (50% inhibitory concentration values of 45.5microM and 11.1microM, respectively), procaine and lidocaine enhanced the inhibitory effect of nondepolarizing muscle relaxants ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143243 Wed, 30 Dec 2009 00:00:00 +0100 3143243 http://www.medworm.com/index.php?rid=3143242&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20045406%26dopt%3DAbstract Authors: Oner SS, Kaya AI, Onaran HO, Ozcan G, Uğur O Membrane rafts and caveolae are specialized microdomains of the cell membrane that form physical platforms for compartmentalization of signalling molecules. Here, we intended to gain insight into the consequences of caveolar localization in G protein-coupled receptor function. We analysed beta(2)-adrenoceptor signalling in purified CRLDF (caveolin-rich low density fractions) of beta(2)-adrenoceptor-overexpressing HEK-293 cells. beta(2)-adrenoceptor and Gs immunoreactivities and forskolin-stimulated adenylate cyclase activity were all detected in CRLDF obtained by the conventional raft purification method that uses Triton X-100 solubilization. However, Triton X-100 caused a complete loss of the functional coupling between beta(... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143242 Wed, 30 Dec 2009 00:00:00 +0100 3143242 http://www.medworm.com/index.php?rid=3143249&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20044987%26dopt%3DAbstract In conclusion, these results indicate that the activation of BK(Ca) channels in VSMCs at least partly contributes to the daidzein-induced vasodilation of the rat cerebral basilar artery. The beta1-subunit of BK(Ca) channels plays a critical role in the activation of BK(Ca) currents by daidzein. PMID: 20044987 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143249 Tue, 29 Dec 2009 00:00:00 +0100 3143249 http://www.medworm.com/index.php?rid=3143248&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20044988%26dopt%3DAbstract Authors: Leffler A, Reckzeh J, Nau C Voltage-gated Na(+) channels (Na(v)) regulate the excitability of sensory neurons and are potential targets for novel analgesics. The secreolytic ambroxol reduces pain-related behavior in rodents and alleviates pain in humans. With properties resembling those of local anesthetics, ambroxol has been reported to block Na(+) currents in sensory neurons with a preference for tetrodotoxin-resistant (TTXr) Na(+) currents encoded by Na(v)1.8. However, the molecular determinants for ambroxol-induced block of Na(+) channels and a preferential block of Na(v)1.8 opposed to tetrodotoxin-sensitive (TTXs) Na(v) alpha-subunits have not been studied in detail. By means of whole-cell voltage clamp recordings, we studied the effects of ambroxol and local anesthetics ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143248 Tue, 29 Dec 2009 00:00:00 +0100 3143248 http://www.medworm.com/index.php?rid=3143247&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20044989%26dopt%3DAbstract In conclusion, GM1 pretreatment, which did not have any effect per se, increased the rewarding effect of cocaine, a phenomenon correlated with a significant increase in the brain cocaine levels. The different pharmacokinetic parameters evaluated, as well as the inhibitory effect of cocaine on the dopamine transporter, were not modified by GM1, but it modifies the brain cocaine disposition. Thus, the mechanisms by which GM1 enhanced the rewarding effects of cocaine merits further study. PMID: 20044989 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143247 Tue, 29 Dec 2009 00:00:00 +0100 3143247 http://www.medworm.com/index.php?rid=3143246&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20044990%26dopt%3DAbstract In conclusion, this study can contribute to elucidate the mechanism responsible for the antioxidant activity of pravastatin, and describes relationship between a scavenger effect of pravastatin and the improvement of vascular reactivity. PMID: 20044990 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143246 Tue, 29 Dec 2009 00:00:00 +0100 3143246 http://www.medworm.com/index.php?rid=3143245&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20044991%26dopt%3DAbstract Authors: Thor D, Uchizono JA, Lin-Cereghino GP, Rahimian R The cardiovascular effects of estrogen are mediated in part by augmenting the function of endothelial nitric oxide synthase. Endothelial nitric oxide synthase activity is dependent on many cofactors including Ca(2+). Hence, we investigated the effect of chronic 17 beta-estradiol treatment on the intracellular Ca(2+) concentration and endothelial nitric oxide synthase protein expression in the human endothelial cell line, EA.hy926, using spectrofluorometry and Western blot, respectively. Inhibiting the sarco(endo)plasmic reticulum Ca(2+) ATPase with thapsigargin caused an increase in the intracellular Ca(2+) concentration, which was higher in chronically 17 beta-estradiol-treated (1muM, 24h) cells loaded with Fura-2-acetoxymethy... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3143245 Tue, 29 Dec 2009 00:00:00 +0100 3143245 http://www.medworm.com/index.php?rid=3136171&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20043903%26dopt%3DAbstract Authors: Lever R, Smailbegovic A, Page CP Heparin is known to possess anti-inflammatory properties that in many cases appear to be separable from its anticoagulant activity. Mast cells, located in tissue, are the sole source of endogenous heparin, which may be involved in control of the inflammatory response. The majority of studies of the effects of heparin on the inflammatory response, carried out to date, have involved systemic administration and the potential influence of heparin in the site of inflammation has been less clear. In the present study, the effects of locally administered heparin and a non-anticoagulant derivative were investigated on leucocyte accumulation in the inflamed peritoneal cavity and leucocyte-endothelial interactions in the mesenteric microcirculation of th... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3136171 Mon, 28 Dec 2009 00:00:00 +0100 3136171 http://www.medworm.com/index.php?rid=3126955&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20036231%26dopt%3DAbstract In conclusion, baicalin could selectively suppress lung carcinoma and lung metastasis by SOD mimic and HIF-1alpha inhibition. PMID: 20036231 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126955 Wed, 23 Dec 2009 00:00:00 +0100 3126955 http://www.medworm.com/index.php?rid=3126965&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035738%26dopt%3DAbstract Authors: Best L, Brown PD, Sener A, Malaisse WJ Tenidap (5-chloro-2-hydroxy-3-(thiophene-2-carbonyl)indole-1-carboxamide) is a non-steroidal anti-inflammatory and anti-rheumatic drug with several cellular actions including inhibition of anion transport processes. Since other anion transport inhibitors have been shown to inhibit activity of the volume-regulated anion channel (VRAC), the present study investigated the effects of tenidap on activity of this channel in pancreatic beta-cells. Membrane potential, VRAC currents and input conductance were recorded from single rat beta-cells in primary culture using perforated patch, conventional whole-cell and cell-attached configurations of the patch-clamp technique. Relative cell volume was measured using a video-imaging method. Tenidap (0.1... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126965 Tue, 22 Dec 2009 00:00:00 +0100 3126965 http://www.medworm.com/index.php?rid=3126964&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035739%26dopt%3DAbstract Authors: McClean PL, Gault VA, Harriott P, Hölscher C Type 2 diabetes has been identified as a risk factor for patients with Alzheimer's disease. Insulin signalling is often impaired in Alzheimer's disease, contributing to the neurodegenerative process. One potential strategy to help prevent this is the normalisation of insulin signalling in the brain. Therefore, the present study was designed to test the effects of novel enzyme-resistant analogues of the insulin-releasing incretin hormone, glucagon-like peptide 1 (GLP-1). The effects of Liraglutide (Victoza) and other novel GLP-1 analogues were tested on synaptic plasticity (LTP) in area CA1 of the hippocampus. At a dose of 15nmol in 5microl i.c.v., Liraglutide (P<0.005), Asp(7)GLP-1 (P<0.001), N-glyc-GLP-1 (P<0.01), and... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126964 Tue, 22 Dec 2009 00:00:00 +0100 3126964 http://www.medworm.com/index.php?rid=3126963&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035740%26dopt%3DAbstract Authors: Roy SJ, Parent A, Gallant MA, De Brum-Fernandes AJ, Stanková J, Parent JL The molecular mechanisms regulating the trafficking of the CRTH2 receptor are poorly understood. In the present study, we characterize C-terminal tail determinants involved in the agonist-induced trafficking of the CRTH2 receptor for prostaglandin D(2). Our results showed that progressive deletion of C-terminal tail residues from amino acid 395 up to 337 gradually impaired CRTH2 internalization by approximately 50% as measured by ELISA in HEK293 cells. Surprisingly, further deletion of the C-tail to amino acid 328 or 317 resulted in receptor mutants displaying internalization similar to the wild-type receptor. Individual mutations of Asp(330), Ser(331), Glu(332), and Leu(333) to Ala in the C-tail of... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126963 Tue, 22 Dec 2009 00:00:00 +0100 3126963 http://www.medworm.com/index.php?rid=3126962&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035741%26dopt%3DAbstract Authors: Ergün Y, Orhan OF, Ozer UG, Gişi G To augment the effects of classical antidepressant drugs by combination therapies in drug-resistant patients has been an emerging treatment strategy. In the present study, the potential synergistic effect of [1H-[1,2,4]Oxadiazole[4,3-a]quinoxalin-1-one] (ODQ) and antidepressant drugs in the forced swimming test was evaluated. While 5mg/kg intraperitoneal administration of imipramine, fluoxetine or desipramine caused no effect in the duration of immobility in the forced swimming test (sub-effective doses), higher doses (20, 10 and 10mg/kg, respectively) reduced the immobility period (effective doses). When sub-effective doses of ODQ (15mg/kg) and imipramine (5mg/kg) were applied, there was a significant reduction in the immobility t... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126962 Tue, 22 Dec 2009 00:00:00 +0100 3126962 http://www.medworm.com/index.php?rid=3126961&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035742%26dopt%3DAbstract Authors: Uzbay T, Kose A, Kayir H, Ulusoy G, Celik T In mammalian brain, agmatine is an endogenous amine that is synthesized through the decarboxylation of L-arginine by arginine decarboxylase. It has been proposed as a new neurotransmitter and/or neuromodulator. It was shown that agmatine had some beneficial effects in animal models of opioid and alcohol addiction. Locomotor stimulant properties of drugs such as ethanol, caffeine, nicotine and amphetamine have been linked to their addictive properties. The present study investigates the effects of agmatine on caffeine-induced locomotor activity both in male and female mice. Adult Swiss Webster mice were used in the study. Locomotor activity was measured for 30min immediately following caffeine (2.5, 5, 10 and 20mg/kg, i.p.) or saline ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126961 Tue, 22 Dec 2009 00:00:00 +0100 3126961 http://www.medworm.com/index.php?rid=3126960&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035743%26dopt%3DAbstract Authors: Rutschow S, Leschka S, Westermann D, Puhl K, Weitz A, Ladyszenskij L, Jaeger S, Zeichhardt H, Noutsias M, Schultheiss HP, Tschope C, Pauschinger M Enteroviruses, especially Coxsackie B3 virus (CVB-3), cause acute viral myocarditis, but the detailed mechanisms leading to chronic left ventricular dysfunction and dilatation remain elusive. Myocardial tissues of CVB-3 infected and sham infected male swr/J mice were analyzed after hemodynamic evaluation on days 4, 7, and 28 p.i. by RT-PCR, gelatin zymography, ELISA, immunohisto-chemistry, sirius red staining, and luxol fast blue staining. In the early phase after infection an abnormal diastolic function was the main hemodynamic finding. CVB-3 infection caused impairment of left ventricular function combined with ventricular dilatat... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126960 Tue, 22 Dec 2009 00:00:00 +0100 3126960 http://www.medworm.com/index.php?rid=3126959&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035744%26dopt%3DAbstract Authors: Tsiklauri N, Viatchenko-Karpinski V, Voitenko N, Tsagareli MG It has recently been shown that antinociceptive tolerance develops by repeated systemic administration of non-steroidal anti-inflammatory drugs (NSAIDs) metamizol and lysine-acetylsalicylate. This is similar to the tolerance observed with opioid-induced analgesia [Vanegas, Tortorici, 2002, Cell and Mol. Neurobiol. 22, 655-661]. In the present study, we investigated the development of tolerance to the analgesic effects of the additional NSAIDs analgine, ketorolac and xefocam in juvenile and adult rats. After injection of each drug, tail flick latencies were significantly elevated on the first day followed by a progressive decrease in tail-flick latency (i.e., tolerance) over the 5-day period, as well as cross-toleran... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126959 Tue, 22 Dec 2009 00:00:00 +0100 3126959 http://www.medworm.com/index.php?rid=3126958&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035745%26dopt%3DAbstract Authors: Chávez-Piña AE, Tapia-Álvarez GR, Navarrete A Hydrogen sulfide (H(2)S) is a gaseous mediator involved in a multitude of physiological functions; however the role of H(2)S in the gut is far from being understood completely. The aim of this study was determine the effect of D,L-propargylglycine (PAG), an inhibitor of H(2)S synthesis, on ethanol-induced gastric injury in rat and to examine the role of L-cysteine, exogenous H(2)S, prostaglandins, non protein sulphydryls groups, nitric oxide and K(ATP) channels in the gastroprotective effect of PAG. Administration of PAG (3.12 to 75mg/kg i.p.) or L-cysteine (0.3 to 300mg/kg, p.o.) exhibited a dose-dependent protective effect after intragastric administration of 1ml of ethanol to induce gastric injury. The gastroprote... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126958 Tue, 22 Dec 2009 00:00:00 +0100 3126958 http://www.medworm.com/index.php?rid=3126957&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035746%26dopt%3DAbstract In conclusion, the loss of the EDHF response may be primarily responsible for the endothelial dysfunction in sepsis, and its restoration by a selective iNOS inhibitor may improve pulmonary vasodilation. PMID: 20035746 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126957 Tue, 22 Dec 2009 00:00:00 +0100 3126957 http://www.medworm.com/index.php?rid=3126956&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20035747%26dopt%3DAbstract In conclusion, edaravone protects rats against acute pancreatitis associated lung injury, probably through its antioxidant and anti-inflammatory effects. Thus, edaravone shows promise as a treatment for lung injury in patients with acute pancreatitis. PMID: 20035747 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3126956 Tue, 22 Dec 2009 00:00:00 +0100 3126956 http://www.medworm.com/index.php?rid=3115848&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20026027%26dopt%3DAbstract Authors: Arib O, Rat P, Molimard R, Chait A, Faure P, de Beaurepaire R It has been suggested that the beta-carbolines harmane and norharmane may be involved in the pathophysiology of Parkinson's disease, psychosis and addiction, but the mechanisms of these possible effects remain to be elucidated. In the present study, the effects of the two compounds were examined by using in vivo extracellular recordings of ventral tegmental dopamine neurons. The effects of harmane (2mg/kg) and norharmane (2mg/kg), were compared to those of nicotine (11microg/kg), of cotinine (0.5mg/kg), of the monoamine-oxidase-A inhibitor befloxatone (0.12mg/kg), and of the monoamine-oxidase-B inhibitor selegiline (0.5mg/kg). The effects of harmane were also tested after pretreatment with the nicotine receptor anta... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3115848 Wed, 16 Dec 2009 00:00:00 +0100 3115848 http://www.medworm.com/index.php?rid=3101154&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20004189%26dopt%3DAbstract This study assessed whether 17beta-estradiol exerts anti-arrhythmic effects through enhanced Connexin43 (Cx43) expression after infarction. Two weeks after ovariectomy, female Wistar rats were randomly assigned to coronary artery ligation or sham-operation. Twenty-four hours after coronary ligation, ovariectomized rats were randomized into vehicle, subcutaneous estradiol treatment, tamoxifen, or subcutaneous estradiol treatment+tamoxifen and followed for 4weeks. To verify the role of estradiol-related nitric oxide in modulating the expression of Cx43, N-nitro-L-arginine methyl ester was also assessed in an in vitro study. Myocardial Cx43 expression revealed a significant decrease in vehicle-treated infarcted rats compared with sham-operated rats at 24h and 4weeks after infarction. Attenuat... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101154 Sat, 12 Dec 2009 00:00:00 +0100 3101154 http://www.medworm.com/index.php?rid=3101153&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20004190%26dopt%3DAbstract Authors: Dai JM, Syyong H, Navarro-Dorado J, Redondo S, Alonso M, van Breemen C, Tejerina T In many vascular smooth muscle cells, physiological and pharmacological agonists initiate oscillatory fluctuations in intracellular Ca(2+) to initiate and maintain vasoconstriction. These oscillations are supported by the underlying cellular ultrastructure, particularly the close apposition between the plasma membrane (PM) and superficial sarcoplasmic reticulum (SR), the so-called PM-SR junctions, which are important for SR Ca(2+) refilling. We hypothesize that the disappearance of PM-SR junctions during aging and/or disease is directly related to the disappearance of agonist-induced Ca(2+) oscillations. We compared phenylephrine-mediated Ca(2+) signals and contraction in human and murine smooth... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101153 Sat, 12 Dec 2009 00:00:00 +0100 3101153 http://www.medworm.com/index.php?rid=3101143&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006961%26dopt%3DAbstract Authors: Takakura K, Fujimori A, Chikanishi T, Tanokura A, Iwatsuki Y, Yamamoto M, Nakajima H, Okada M, Itoh H Renal fibrosis is the final common pathway of chronic kidney disease, and its progression predicts the degree of renal dysfunction. We investigated the renoprotective properties of pirfenidone in a remnant kidney model of chronic renal failure to determine its pharmacological potency compared to enalapril. Five-sixths-nephrectomized rats were fed diet containing pirfenidone (approximately 700mg/kg/day) for 8weeks. Pirfenidone steadily inhibited the progression of proteinuria, but not to a significant degree. Pirfenidone prevented the elevation of plasma creatinine and blood urea nitrogen. At the end of the experiment, pirfenidone had reduced systolic blood pressure by means of... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101143 Sat, 12 Dec 2009 00:00:00 +0100 3101143 http://www.medworm.com/index.php?rid=3101142&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006962%26dopt%3DAbstract Authors: Villa FA, Lieske K, Gerwick L In response to evolutionary selective pressure, prokaryotes have developed a rich array of secondary metabolites, some of which may be inhibitory to the innate immune system and the inflammatory response in vertebrates. We utilized the RAW264.7 macrophage cell line stimulated with LPS in a nitric oxide (NO) assay to screen for compounds with immunomodulatory activities from a library of marine natural products, and found that the malyngamide structure class, found commonly in the marine cyanobacterium Lyngbya majuscula, has potent activity. Several of the malyngamides were found to possess IC50 values of 5.4 - 18microM. Malyngamide F acetate exhibited strong concentration-dependent anti- inflammatory activity in the NO assay with an IC50 of 7.1mic... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101142 Sat, 12 Dec 2009 00:00:00 +0100 3101142 http://www.medworm.com/index.php?rid=3101141&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006963%26dopt%3DAbstract Authors: Yuan XY, Liu W, Zhang P, Wang RY, Guo JY Allergic contact dermatitis is a prototypic T-cell-mediated cutaneous inflammatory response. Multiple cell types, inflammatory mediators and cytokines are involved in the regulation of immunologic and inflammatory processes in allergic contact dermatitis. Aloperine is an isolated alkaloid found in the plant of Sophora alopecuroides L. It has been clinically proved effective in China for a long time for skin inflammatory diseases such as allergic contact dermatitis. However, the mechanism of aloperine on allergic contact dermatitis is largely unknown. Therefore, the aim of this study was to investigate the effect of aloperine on 2, 4- dinitrofluorobenzene (DNFB) induced-allergic contact dermatitis in BALB/c mice and the possible underlyi... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101141 Sat, 12 Dec 2009 00:00:00 +0100 3101141 http://www.medworm.com/index.php?rid=3101150&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006596%26dopt%3DAbstract We describe the pharmacological and pharmacokinetic profile of SCH 486757, a nociceptin/orphanin FQ peptide (NOP) receptor agonist that has recently entered human clinical trials for cough. SCH 486757 selectively binds human NOP receptor (Ki=4.6+/-0.61 nM) over classical opioid receptors. In a guinea pig capsaicin cough model, SCH 486757 (0.01 - 1mg/kg) suppressed cough at 2, 4, and 6 hours post oral administration with a maximum efficacy occurring at 4hrs equivalent to codeine, hydrocodone, dextromethorphan and baclofen. The antitussive effects of SCH 486757 (3.0mg/kg, p.o.) was blocked by the NOP receptor antagonist J113397 (12mg/kg, i.p.) but not by naltrexone (10mg/kg, p.o.). SCH 486757 does not produce tolerance to its antitussive activity after a 5day BID dosing regimen. After acute ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101150 Fri, 11 Dec 2009 00:00:00 +0100 3101150 http://www.medworm.com/index.php?rid=3101149&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006597%26dopt%3DAbstract Authors: Kittler K, Lau T, Schloss P The serotonin transporter (SERT) terminates serotonergic neurotransmission by the rapid removal of serotonin (5-hydroxytryptamine, 5-HT) from the extracellular space back into serotonergic neurons. SERT therefore controls the concentration of extracellular 5-HT, and thus one mechanism to regulate the efficacy of serotonergic neurotransmission is via modulation of the density of SERT molecules on the cell membrane. We have studied effects of prolonged exposure to various selective serotonin re-uptake inhibitors (SSRIs), as well as cocaine and the transport substrates 5-HT and 3,4-methylenedioxy-methamphetamine (MDMA), on SERT cell surface expression in cultured serotonergic neurons. This was achieved via quantification of the amount of cell surface-e... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101149 Fri, 11 Dec 2009 00:00:00 +0100 3101149 http://www.medworm.com/index.php?rid=3101148&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006598%26dopt%3DAbstract Authors: Chen X, Pi R, Zou Y, Liu M, Ma X, Jiang Y, Mao X, Hu X Osthole, a natural coumarin, is known to have a variety of pharmacological and biochemical uses and is considered to have potential therapeutic applications. Here we examined the effects of osthole on the central nervous system demyelination in experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis and its mechanism(s). C57 BL/6 mice immunized with myelin oligodendrocyte glycoprotein 35-55 amino acid peptide were treated with osthole at day 7 post immunization (7 p.i., subclinical periods, early osthole treatment) and day 13 p.i. (clinical periods, late osthole treatment) respectively and both therapies continued throughout the study. The content of nerve growth factor (NGF) and interferon gamma (IF... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101148 Fri, 11 Dec 2009 00:00:00 +0100 3101148 http://www.medworm.com/index.php?rid=3101147&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006599%26dopt%3DAbstract Authors: El Gebeily G, Fiset C Tamoxifen is a widely used chemotherapeutic agent, which has been associated with prolongation of the QT interval. Other studies have reported that acute exposure to tamoxifen can reduce cardiac K(+) currents. However, in vivo tamoxifen is largely metabolized and most of its activity is attributable to its major metabolite, 4-hydroxytamoxifen (4OH-tamoxifen). Accordingly, in the present study, we performed voltage-clamp experiments to directly investigate the effects of 4OH-tamoxifen on the repolarizing K(+) currents in adult mouse ventricular myocytes in order to determine whether the effects of tamoxifen on repolarization could be ascribed to 4OH-tamoxifen. K(+) currents were recorded before and after acute exposure to 4OH-tamoxifen (0.5, 1 and 10muM). ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101147 Fri, 11 Dec 2009 00:00:00 +0100 3101147 http://www.medworm.com/index.php?rid=3101146&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006600%26dopt%3DAbstract Authors: Roland JJ, Levinson M, Vetreno RP, Savage LM Several lines of evidence suggest that acetylcholinesterase inhibitors (AChE) inhibitors have their cognitive enhancing effects by stimulating cholinergic receptors within the medial septum. However, intraseptal administration of cholinergic enhancing drugs produce mixed results that appear to depend on both the integrity of the medial septum as well as task demands. Three experiments were conducted to determine the relationship between increased cholinergic activity within the medial septum and hippocampus and behavioral recovery in a model of diencephalic amnesia produced by pyrithiamine-induced thiamine deficiency (PTD). In Experiment 1, systemic tacrine (0.0, 0.75, 1.5mg/kg) was administered to PTD and pair-fed (PF) rats prior t... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101146 Fri, 11 Dec 2009 00:00:00 +0100 3101146 http://www.medworm.com/index.php?rid=3101145&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006601%26dopt%3DAbstract We examined the role of ADAMTS-1 in the antifibrotic activity of the ACE inhibitor Captopril in a chronic viral myocarditis (CVMC) model. Balb/c mice were assigned to five groups: normal control group1 (group 1) , normal control group2 (group 2), CVMC model group(group 3), CVMC control group (group 4) and Captopril therapy group (group 5) . Group 3, 4 and 5 received Coxsackievirus B(3) to induce CVMC and group 5 was treated with Captopril (100mg/kg )for 28days. Heart sections were stained with picrosirius red and collagen volume fraction calculated. ADAMTS-1 expression was determined by Western blot. Type I collagen and carboxyterminal telopeptide of type I collagen (ICTP) were measured by RT- PCR. Group 4 mice had significantly increased collagen volume fraction compared to groups 2 and 5... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101145 Fri, 11 Dec 2009 00:00:00 +0100 3101145 http://www.medworm.com/index.php?rid=3101144&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20006602%26dopt%3DAbstract Authors: El-Hashim A, Yousefi S, Edafiogho I, Raghupathy R, Yousif M, Simon HU Asthma is a chronic inflammatory disease of the airways. The treatment of asthma is far from optimal and hence the need for novel therapeutic agents exists. The purpose of this study was to assess the anti-asthma effects of an enaminone, E121, and also its effects on human peripheral blood mononuclear cell proliferation and cytokine release. The effects of E121 were assessed in an ovalbumin-induced model of airway inflammation and airway hyperresponsiveness. In addition, the effects of E121 on phytohemagglutinin (PHA), anti-CD3 monoclonal antibody and lipopolysaccharide (LPS)-induced human peripheral blood mononuclear cell proliferation and cytokine release, respectively, were assessed. Treatment of mice wit... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101144 Fri, 11 Dec 2009 00:00:00 +0100 3101144 http://www.medworm.com/index.php?rid=3101152&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20004657%26dopt%3DAbstract Authors: Liu X, Luo D, Zheng M, Hao Y, Hou L, Zhang S Insulin resistance, which may influence Alzheimer's disease, is associated with an increase in circulating advanced glycosylation end products (AGEs) and the increased expression of the receptor for AGEs (RAGE). Inhibition of AGE/RAGE system has been shown to attenuate neuronal damage. Specific ligands for peroxisome proliferator-activated receptorgamma (PPARgamma), which have proven effective in the animal models of Alzheimer's disease and other neuroinflammatory diseases, has been shown to decrease RAGE expression. Here we investigated the effect of PPARgamma agonist, pioglitazone, on cognition function and AGE/RAGE system in a rodent model of insulin resistance, the fructose-drinking rats. Six-week-old male Wistar rats were fed a... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101152 Wed, 09 Dec 2009 00:00:00 +0100 3101152 http://www.medworm.com/index.php?rid=3101151&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D20004658%26dopt%3DAbstract Authors: Olivier JD, Cools AR, Deen PM, Olivier B, Ellenbroek BA To investigate whether life-long disturbed serotonin neurotransmission may result in adaptive changes of dopaminergic and noradrenergic systems, effects of drugs on stress-induced hyperthermia were studied in serotonin transporter knockout rats. The noradrenalin transporter blocker atomoxetine was more effective in reducing stress-induced hyperthermia, induced by an injection, in serotonin transporter (SERT) knockout (SERT(-/-)) rats compared to SERT(+/+) rats. The dopamine transporter blocker GBR12909 increased the core body temperature in SERT(-/-) rats, and had no effect on the SERT(+/+) rats. Finally, the noradrenalin transporter together with dopamine transporter blocker bupropion was more effective in decreasing the... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3101151 Tue, 08 Dec 2009 00:00:00 +0100 3101151 http://www.medworm.com/index.php?rid=3067996&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19962976%26dopt%3DAbstract Authors: Hu L, Sun Y, Hu J Catalpol, an iridoid glucoside found in the root of Rehmannia glutinosa Libosch, has been demonstrated to reduce apoptosis in neuronal cell lines. Recent data suggests that catalpol also exerts anti-apoptotic effects on other cell types. The aim of the present study was to investigate whether catalpol protects against hydrogen peroxide (H(2)O(2)) induced apoptosis in human umbilical vein endothelial cells (HUVECs). Apoptotic cells were detected by terminal deoxyribonucleotidyl transferase-mediated deoxyuridine triphosphate-biotin nick end labeling, Annexin V-fluorescein isothiocyanate binding assay and by assessment of caspase-3 activity. The level of intracellular reactive oxygen species were quantified by 2', 7' -dichlorofluorescein diacetate assay. Express... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3067996 Thu, 03 Dec 2009 00:00:00 +0100 3067996 http://www.medworm.com/index.php?rid=3067995&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19962977%26dopt%3DAbstract Authors: Geraets L, Haegens A, Weseler AR, Brauers K, Vernooy JH, Wouters EF, Bast A, Hageman GJ The nuclear enzyme poly(ADP-ribose) polymerse-1 (PARP-1) has previously been reported to play an important role in lipopolysaccharide (LPS)-induced pulmonary inflammation and is highly activated in COPD patients. In the present study, the anti-inflammatory efficacy of a previously identified poly(ADP-ribose) polymerase-1 (PARP-1) inhibiting caffeine metabolite, 1,7-dimethylxanthine, was both in vivo as well as ex vivo evaluated. Orally administered 1,7-dimethylxanthine significantly attenuated lung myeloperoxidase-levels, transcription of IL-6, TNF-alpha, MIP1alpha and MIP2 genes as well as PAR-polymer formation in a mouse model of intratracheally LPS-induced acute pulmonary inflammation. S... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3067995 Thu, 03 Dec 2009 00:00:00 +0100 3067995 http://www.medworm.com/index.php?rid=3067999&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19961845%26dopt%3DAbstract In conclusion, mizoribine and ribavirin were found to be absorbed efficiently to the same extents from the whole small intestine. Also, the altered gastric emptying rates exerted no significant effects on the oral bioavailabilities of mizoribine and ribavirin. PMID: 19961845 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3067999 Tue, 01 Dec 2009 00:00:00 +0100 3067999 http://www.medworm.com/index.php?rid=3067998&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19961846%26dopt%3DAbstract Authors: Nakamura K, Yokotani K Previously, we reported that prostanoid TP receptor mediates the inhibition of electrically evoked noradrenaline release from gastric sympathetic nerves in rats. Prostanoid TP receptor has been shown to activate phospholipase C (PLC), which catalyzes the hydrolysis of phosphatidylinositol 4,5-bisphosphate to inositol 1,4,5-triphosphate (IP(3)) and diacylglycerol; IP(3) triggers the release of Ca(2+) from intracellular stores and diacylglycerol activates protein kinase C. In the present study, therefore, we examined whether these PLC-mediated mechanisms are involved in the TP receptor-mediated inhibition of gastric noradrenaline release using an isolated, vascularly perfused rat stomach. U-46619 (9,11-dideoxy-9alpha,11alpha-methanoepoxy PGF(2alpha)) (a pr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3067998 Tue, 01 Dec 2009 00:00:00 +0100 3067998 http://www.medworm.com/index.php?rid=3067997&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19961847%26dopt%3DAbstract Authors: Jiang WL, Fu FH, Zheng SG, Zhang DL, Zhu HB, Jian-Hou 8-O-acetyl shanzhiside methylester (ND01), an iridoid glucoside compound, was isolated from the leaves of Lamiophlomis rotata (Benth.) Kudo. The present study elucidated the effects of ND01 on the cultured rat cortical neurons injury induced by oxygen-glucose deprivation. The results showed that ND01 treatment obviously attenuated apoptosis and ameliorated mitochondrial energy metabolism in rat cortical neurons by increasing cell survival rate, mitochondrial respiratory enzymes activities, mitochondrial respiratory control ratio and adenosine triphosphate (ATP) content, and by attenuating lactate dehydrogenase (LDH) leakage, intracellular Ca(2+) level and caspase-3 activity in a concentration-dependent manner. These findin... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3067997 Tue, 01 Dec 2009 00:00:00 +0100 3067997 http://www.medworm.com/index.php?rid=3059937&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958757%26dopt%3DAbstract Authors: Huang KF, Huang WT, Lin KC, Lin MT, Chang CP The present study was attempted to determine whether interleukin-1 receptor antagonist (IL-1ra) pretreatment exerts its anti-pyresis by reducing organum vasculosum laminae terminalis (OVLT) release of glutamate, hydroxyl radicals and prostaglandin-E(2) in rabbits. It was found that systemic administration of lipopolysaccharide induced increased levels of both core temperature and OVLT levels of glutamate, hydroxyl radicals, and prostaglandin E(2). The rise in both the core temperature and OVLT glutamate, hydroxyl radicals and prostaglandin E(2) could also be induced by intracerebroventricular injection of interleukin-1beta. Pretreatment with an intracerebroventricular dose of IL-1ra significantly prevented the lipopolysaccharide or ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059937 Mon, 30 Nov 2009 00:00:00 +0100 3059937 http://www.medworm.com/index.php?rid=3059936&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958758%26dopt%3DAbstract Authors: Sugimoto Y, Furutani S, Kajiwara Y, Hirano K, Yamada S, Tagawa N, Kobayashi Y, Hotta Y, Yamada J We previously demonstrated the presence of strain differences in baseline immobility time and sensitivity to the selective serotonin reuptake inhibitor (SSRI) fluvoxamine in five strains of mice (ICR, ddY, C57BL, DBA/2 and BALB/c mice). Furthermore, variations in serotonin (5-HT) transporter binding in the brain were strongly related to strain differences in baseline immobility and sensitivity to fluvoxamine. In the present study, we examined the involvement of the 5-HT(1A) receptor in anti-immobility effects in DBA/2 mice, which show high sensitivity to fluvoxamine. The anti-immobility effects of fluvoxamine in DBA/2 mice were inhibited by the 5-HT(1A) receptor antagonist N-[2-[4-... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059936 Mon, 30 Nov 2009 00:00:00 +0100 3059936 http://www.medworm.com/index.php?rid=3059935&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958759%26dopt%3DAbstract Authors: Sidhu S, Pandhi P, Malhotra S, Vaiphei K, Khanduja KL Current treatment options for acute pancreatitis are supportive and symptomatic. Due to lack of agents targeting the underlying pathophysiology a large amount of experimental work is going on to identify novel therapeutic agents. The present study was carried out to explore if melatonin can modulate the spontaneous regeneration process of the pancreas after experimentally induced acute pancreatitis. Rats were given two i.p. injections of L-arginine in a dose 200mg/100g at an interval of 1h for induction of pancreatitis. After this rats were randomly divided into three groups i.e. saline, CCK-8 and melatonin. Drug treatment was started 2h after the last L-arginine injection and continued till day of sacrifice. An additional ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059935 Mon, 30 Nov 2009 00:00:00 +0100 3059935 http://www.medworm.com/index.php?rid=3059934&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958760%26dopt%3DAbstract Authors: Ambroziak K, Kuteykin-Teplyakov K, Luna-Tórtos C, Al-Falah M, Fedrowitz M, Löscher W Several major antiepileptic drugs, including carbamazepine, phenytoin and phenobarbital, induce xenobiotic metabolizing enzymes via activation of nuclear receptors, including pregnane X receptor (NR1I2) and constitutive androstane receptor (NR1I3). Via activation of these xenobiotic sensors, antiepileptic drugs may also induce the expression of efflux transporters such as P-glycoprotein (Pgp) in different tissues, including intestine, liver, kidney and brain. Increased expression of Pgp in brain capillary endothelial cells, which form the blood-brain barrier, could limit the penetration of antiepileptic drugs into the brain and therefore decrease their therapeutic efficacy. As a cons... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059934 Mon, 30 Nov 2009 00:00:00 +0100 3059934 http://www.medworm.com/index.php?rid=3059933&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958761%26dopt%3DAbstract We examined the effects of physalaemin, an agonist of tachykinin receptors, on mechanical responses in the rat esophagus to clarify possible regulatory roles of tachykinins in esophageal motility. Exogenous application of physalaemin caused tonic contractions in rat esophageal segments when tension was recorded in the longitudinal direction but not when tension was recorded in the circular direction. The physalaemin-evoked contractions were blocked by pretreatment with nifedipine, a blocker of L-type calcium channels in both striated and smooth muscle cells. However, tetrodotoxin, a blocker of voltage-dependent sodium channels in striated muscle cells and neurons, did not affect the physalaemin-induced contractions. These results indicate that physalaemin might induce contractile responses... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059933 Mon, 30 Nov 2009 00:00:00 +0100 3059933 http://www.medworm.com/index.php?rid=3059932&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958762%26dopt%3DAbstract Authors: Wakabayashi I, Nakano T, Takahashi Y The purpose of this study was to determine whether expression of inducible nitric oxide synthase (iNOS) is altered in vascular smooth muscle cells of type 2 diabetes rats. We used cultured aortic smooth muscle cells (ASMCs) isolated from male Goto-Kakizaki diabetes rats (G-K rats) aged 27 - 28weeks and age-matched Wistar rats (control rats). iNOS and extracellular signal-regulated kinase (ERK) were evaluated by immunoblot and/or immunochemical analyses, and NO production was evaluated by measuring NO(X) (NO(2) and NO(3)). Expression of iNOS was not detected in ASMCs of either G-K or control rats under a resting condition. Stimulation with interleukin-1beta (IL-1beta) induced iNOS expression, which was much greater in ASMCs from G-K rats tha... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059932 Mon, 30 Nov 2009 00:00:00 +0100 3059932 http://www.medworm.com/index.php?rid=3059931&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958763%26dopt%3DAbstract Authors: Jiang SX, Zheng RY, Zeng JQ, Li XL, Han Z, Hou ST Intracellular calcium ([Ca(2+)]i) influx through N-methyl-D-aspartic acid (NMDA) receptors in cortical neurons is central to NMDA receptor-mediated excitotoxicity. Drugs that uncompetitively modulate NMDA receptor-mediated [Ca(2+)]i influx are potential leads for development to treat NMDA receptor-mediated neuronal damage since these drugs spare NMDA receptor normal functions. Ligands to alpha(2)-adrenoceptors and imidazoline I(2) receptors confer neuroprotection possibility through modulating NMDA receptor-mediated [Ca(2+)]i influx. Here, we investigated the characteristics of several ligands to alpha(2)-adrenoceptors and imidazoline I(2) receptor, in inhibiting NMDA receptor-mediated [Ca(2+)]i influx in cultured cortical neur... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059931 Mon, 30 Nov 2009 00:00:00 +0100 3059931 http://www.medworm.com/index.php?rid=3059930&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958764%26dopt%3DAbstract Authors: Tham CL, Liew CY, Lam KW, Mohamad AS, Kim MK, Cheah YK, Zakaria ZA, Sulaiman MR, Lajis NH, Israf DA Curcumin is a highly pleiotropic molecule with significant regulatory effects upon inflammation and inflammatory related diseases. However curcumin has one major important limitation in which it has poor bioavailability. Design of synthetic structural derivatives of curcumin is but one approach that has been used to overcome its poor bioavailability while retaining, or further enhancing, its drug-like effects. We have synthesized a series of curcumin analogues and describe the effects of 2,6-bis-4-(hydroxyl-3-methoxy-benzylidine)-cyclohexanone or BHMC upon nitric oxide and cytokine synthesis in cellular models of inflammation. BHMC showed a significant dose-response inhibitory a... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059930 Mon, 30 Nov 2009 00:00:00 +0100 3059930 http://www.medworm.com/index.php?rid=3059929&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958765%26dopt%3DAbstract Authors: Szőke E, Börzsei R, Tóth DM, Lengl O, Helyes Z, Sándor Z, Szolcsányi J The transient receptor potential vanilloid 1 (TRPV1) is a noxious heat-sensitive, chemonociceptive cation channel which is expressed in primary sensory neurons of polymodal nociceptors. The present study is devoted to analyse the role of lipid raft constituents in calcium influx evoked by various TRPV1 agonists on sensory neurons and on rTRPV1-transfected CHO cell line. Depletion of cholesterol by methyl beta-cyclodextrin (MCD, 1-10mM) diminished the percent of the calcium uptake response of cultured trigeminal neurons to capsaicin (100nM) or resiniferatoxin (RTX, 3nM). In contrast, in TRPV1-transfected cells the inhibition was observed only when capsaicin or N-oleoyldopamine (OLDA... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059929 Mon, 30 Nov 2009 00:00:00 +0100 3059929 http://www.medworm.com/index.php?rid=3059928&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958766%26dopt%3DAbstract Authors: Adeleye A, Shohami E, Nachman D, Alexandrovich A, Trembovler V, Yaka R, Shoshan Y, Dhawan J, Biegon A It has been long thought that hyper-activation of N-methyl-D-aspartate (NMDA) receptors underlies neurological decline after traumatic brain injury. However, all clinical trials with NMDA receptor antagonists failed. Since NMDA receptors are down-regulated from 4h to 2weeks after brain injury, activation at 24h, rather than inhibition, of these receptors, was previously shown to be beneficial in mice. Here, we tested the therapeutic window, dose regimen and mechanism of action of the NMDA receptor partial agonist D-cycloserine (DCS) in traumatic brain injury. Male mice were subjected to trauma using a weight-drop model, and administered 10mg/kg (i.p) DCS or vehicle once (8, 16... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059928 Mon, 30 Nov 2009 00:00:00 +0100 3059928 http://www.medworm.com/index.php?rid=3059927&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958767%26dopt%3DAbstract In conclusion, oxygen/ozone has antiarrhythmic effects against arrhythmias caused by aconitine, myocardial ischemia and ischemia/reperfusion. PMID: 19958767 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059927 Mon, 30 Nov 2009 00:00:00 +0100 3059927 http://www.medworm.com/index.php?rid=3059926&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958768%26dopt%3DAbstract Authors: van Oostrom H, Stienen PJ, Doornenbal A, Hellebrekers LJ It was investigated whether continuous rate infusion of the alpha(2)-adrenoceptor agonist dexmedetomidine can suppress memory formation by mechanisms other than reducing perception of sensory input in a fear-conditioning paradigm. Different groups of rats infused with either saline or dexmedetomidine (2.0, 4.0 or 10.0microg/kg bolus, followed by 2.0, 4.0 or 10.0microg/kg/h continuous rate infusion respectively), were subjected to a somatosensory-evoked potential (SEP) fear-conditioning paradigm. This paradigm combined the pairing of an innoxious conditioned stimulus (CS) and a noxious unconditioned stimulus (US), of which the latter was used to generate the SEPs (training phase).The following day, the perception of the U... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059926 Mon, 30 Nov 2009 00:00:00 +0100 3059926 http://www.medworm.com/index.php?rid=3059925&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19958769%26dopt%3DAbstract Authors: Chatzikyriakou SV, Tziakas DN, Chalikias GK, Stakos D, Thomaidi A, Mitrousi K, Boudoulas H Not all patients respond to angiotensin converting enzyme (ACE) - inhibitor equally. Genetic or other phenotypic variations might be useful in predicting the therapeutic efficacy of these drugs. With the present study we assessed the prognostic impact of ACE- inhibitor in chronic heart failure patients with different degree of collagen metabolism as assessed by serum levels of a collagen type-I degradation marker (CITP). 196 (126 male, 69+/-10years) chronic heart failure patients were studied prospectively for 12months regarding survival. Serum concentrations of CITP were measured at study entry. Chronic heart failure patients were divided into groups according to whether (n=114) or not ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3059925 Mon, 30 Nov 2009 00:00:00 +0100 3059925 http://www.medworm.com/index.php?rid=3052814&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19948164%26dopt%3DAbstract In this study, twelve month old male mice were chronically treated for 21days with stress-level dexamethasone (5mg/kg). We investigated the pathological consequences of dexamethasone administration on learning and memory impairments, amyloid precursor protein processing and neuronal cell apoptosis in 12-month old male mice. Our results indicate that dexamethasone can induce learning and memory impairments, neuronal cell apoptosis, and mRNA levels of the amyloid precursor protein, beta-secretase and caspase-3 are selectively increased after dexamethasone administration. Immunohistochemistry demonstrated that amyloid precursor protein, caspase-3 and cytochrome c in the cortex and CA1, CA3 regions of the hippocampus are significantly increased in 12-month old male mice. Furthermore, dexametha... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3052814 Fri, 27 Nov 2009 00:00:00 +0100 3052814 http://www.medworm.com/index.php?rid=3045254&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19944677%26dopt%3DAbstract Authors: Li R, Zhang H, Wang W, Wang X, Huang Y, Huang C, Gao F It is well known that systemic insulin resistance is closely associated with the metabolic syndrome including type 2 diabetes and hypertension. However, it remains unclear whether vascular insulin resistance acts as an early etiologic factor for the development of hypertension. Male spontaneously hypertensive rats (SHRs) aged 5weeks (young) and 15weeks (adult) were studied and vascular insulin resistance was assessed as the function of isolated aortic vasodilatory response to insulin in vitro. Compared with Wistar-Kyoto (WKY) rats, adult SHRs exhibited significant hypertension with significantly decreased aortic vasodilatation to insulin, whereas young SHRs had normal blood pressure but exhibited similar vascular insulin r... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045254 Thu, 26 Nov 2009 00:00:00 +0100 3045254 http://www.medworm.com/index.php?rid=3045249&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19945453%26dopt%3DAbstract Authors: Currò D Ca(2+) inflow responsible for neurotransmitter release at most peripheral junctions is mainly mediated by activation of Ca(V)2.2 and Ca(V)2.1 channels. The aim of the present study was to characterize the voltage-gated Ca(2+) channels (VGCCs) responsible for the non-adrenergic non-cholinergic (NANC) relaxation and vasoactive intestinal polypeptide (VIP)-like immunoreactivity release in the rat gastric fundus. Precontracted longitudinal muscle strips of the rat gastric fundus were subjected to electrical field stimulation (EFS) under NANC conditions to evoke the relaxation and VIP-like immunoreactivity release. Nifedipine (1microM) completely relaxed the preparations, so that its effects on EFS-induced NANC relaxations could not be investigated. omega-Conotoxin GVI... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045249 Thu, 26 Nov 2009 00:00:00 +0100 3045249 http://www.medworm.com/index.php?rid=3045248&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19945454%26dopt%3DAbstract Authors: Kociecka B, Surazynski A, Miltyk W, Palka J PPAR- gamma and estrogen receptor belong to a family of nuclear hormone receptors that were shown to affect transcriptional activity of each other. The angiotensin II type 1 receptor antagonist Telmisartan is well known PPAR- gamma ligand. The effect of Telmisartan-induced PPAR- gamma activation on collagen biosynthesis was studied in the estrogen-dependent (MCF-7 cells expressing alpha and beta receptor) and estrogen-independent (MDA-MB 231, expressing only beta receptor) cell lines. We have found that the presence of estrogen in growth medium (2nM) augmented collagen biosynthesis in both cell lines. An addition to the growth medium of PPAR- gamma agonist, Telmisartan, but not rosiglitazone or clofibrat, other PPAR- gamma agonists, ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045248 Thu, 26 Nov 2009 00:00:00 +0100 3045248 http://www.medworm.com/index.php?rid=3045253&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19944678%26dopt%3DAbstract Authors: Zheng W Emerging evidences recently indicate that anterior cingulate cortex is critically involved in the central processing and modulation of noxious stimulus, although the neuroadaptation in anterior cingulate cortex has not been well documented in the conditions of chronic pain. Meanwhile, the cellular mechanism underlying opiates analgesia in anterior cingulate cortex remains unclear. To address these issues, the present study was undertaken to explore the adaptation of excitatory glutamatergic transmission and mu opioid receptor-mediated modulation of glutamatergic transmission in the anterior cingulate cortex slices from the complete Freund's adjuvant (CFA) -inflamed rats. The results demonstrated that glutamatergic paired-pulse facilitation was decreased in the anterior... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045253 Wed, 25 Nov 2009 00:00:00 +0100 3045253 http://www.medworm.com/index.php?rid=3045252&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19944679%26dopt%3DAbstract Authors: Yang G, Li T, Xu J, Liu L The present study investigated the mediated effect of protein kinase C (PKC) in arginine vasopressin (AVP) induced restoration of vascular responsiveness and calcium sensitization following hemorrhagic shock. Using both isolated superior mesenteric artery from hemorrhagic shock rats and hypoxia-treated vascular smooth muscle cell (VSMC), we investigated the roles of PKC alpha, delta and epsilon isoforms in AVP induced restoration of vascular reactivity and calcium sensitivity. Meanwhile, effects of their specific inhibitors on the activity of myosin light chain phosphatase (MLCP), myosin light chain kinase (MLCK), and the phosphorylation of myosin light chain (MLC(20)) in VSMC were observed. The results indicated that AVP improved the reactivity of su... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045252 Wed, 25 Nov 2009 00:00:00 +0100 3045252 http://www.medworm.com/index.php?rid=3045251&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19944680%26dopt%3DAbstract We report that the anxiolytic-like effects of fluoxetine correlate in time and amplitude with 5-HT1A autoreceptor desensitization, but neither with the extracellular levels of 5-HT in the raphe nuclei, nor in the hippocampus. Our study suggests that the beneficial anxiolytic/antidepressant-like effects of chronic SSRI treatment indeed depend on 5-HT1A autoreceptor internalization, but do not require a sustained increase in extracellular 5-HT levels in a territory of 5-HT projection such as hippocampus. PMID: 19944680 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045251 Wed, 25 Nov 2009 00:00:00 +0100 3045251 http://www.medworm.com/index.php?rid=3045250&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19944681%26dopt%3DAbstract In conclusion, diabetes mitigated remifentanil induced cardioprotection against ischemia-reperfusion, which might be associated with reduced recovery of the activities of proteins involved in anti-apoptotic pathways including ERK1/2 and the abnormal expression of sarcoplasmic reticulum genes as a result of ischemia-reperfusion in rat hearts. PMID: 19944681 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045250 Wed, 25 Nov 2009 00:00:00 +0100 3045250 http://www.medworm.com/index.php?rid=3045255&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19944091%26dopt%3DAbstract Conclusions - These results may help to explain the efficiency of aminoglycoside and anti-dystrophin antisense treatments in smooth muscle. Both treatments could be an interesting therapeutic option to restore smooth muscle contraction in patients with Duchenne muscular dystrophy. PMID: 19944091 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3045255 Tue, 24 Nov 2009 00:00:00 +0100 3045255 http://www.medworm.com/index.php?rid=3037274&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19941848%26dopt%3DAbstract This study is the first to show that some leukotrienes induce emesis, possibly involving both central and peripheral leukotriene CysLT(1) and/or leukotriene CysLT(2) receptors. PMID: 19941848 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3037274 Mon, 23 Nov 2009 00:00:00 +0100 3037274 http://www.medworm.com/index.php?rid=3037273&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19941849%26dopt%3DAbstract Authors: Pagano RL, Sampaio SC, Juliano MA, Juliano L, Giorgi R Proteinase-activated receptors (PAR) are widely recognized for their modulatory properties in inflammatory and immune responses; however, their direct role on phagocyte effector functions remains unknown. S100A9, a protein secreted during inflammatory responses, deactivates activated peritoneal macrophages, and its C-terminal portion inhibits spreading and phagocytosis of adherent peritoneal cells. Herein, the effect of PAR1 and PAR2 agonists was investigated on spreading and phagocytosis by adherent peritoneal cells, as well as the ability of murine C-terminal of S100A9 peptide (mS100A9p) to modulate this effect. Adherent peritoneal cells obtained from mouse abdominal cavity were incubated with PAR1 and PAR2 agonists and ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3037273 Mon, 23 Nov 2009 00:00:00 +0100 3037273 http://www.medworm.com/index.php?rid=3037272&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19941850%26dopt%3DAbstract In this study, we investigated the effects of Cryptomerione on the phenotypic and functional maturation of human monocyte-derived dendritic cells in vitro. Human monocytes were exposed to either Cryptomerione alone, or in combination with lipopolysaccaride (LPS) or cholera toxin (CT) and thereafter co-cultured with naïve T cells. We found no enhanced CD1a, CD80, CD83, CD86 and HLA-DR expression on Cryptomerione-primed dendritic cells. However, Cryptomerione augmented T cell stimulatory capacity in an allogeneic mixed lymphocyte reaction to CT-primed dendritic cells and influenced the production of interleukin (IL)-10 and IL-12p70 by CT-primed dendritic cells, but not LPS-primed dendritic cells. Cryptomerione also inhibited Th2 cell polarization induced by CT-primed dendritic cells, bu... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3037272 Mon, 23 Nov 2009 00:00:00 +0100 3037272 http://www.medworm.com/index.php?rid=3037271&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19941851%26dopt%3DAbstract Authors: Eder K, Ringseis R Former studies in rats demonstrated that starvation or treatment with the hypolipidemic drug clofibrate causes a marked increase in the concentration of carnitine in the liver. The molecular mechanisms underlying these phenomena in rats, however, have been largely unknown. Since both, fasting and clofibrate treatment lead to an activation of peroxisome proliferator-activated receptor alpha (PPARalpha), the hypothesis has been raised that activation of this nuclear receptor could lead to an up-regulation of novel organic cation transporters (OCTN) which facilitate transport of carnitine and several other organic cations through membranes. Studies in rodents and pigs have indeed shown that treatment with PPARalpha agonists causes an up-regulation of OCTN2 in l... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3037271 Mon, 23 Nov 2009 00:00:00 +0100 3037271 http://www.medworm.com/index.php?rid=3027218&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19932884%26dopt%3DAbstract Authors: Li B, Arime Y, Hall FS, Uhl GR, Cui R, Sora I Brain-derived neurotrophic factor (BDNF), one of the key brain neurotrophins, has been implicated in neuronal plasticity and memory. Recent studies document the importance of BDNF for normal long-term memory functions. However, there are few studies of the roles of BDNF in short term memory. Dopamine is likely to play important roles in BDNF gene expression in specific brain regions, including frontal cortical regions that are implicated in short term working memory processes that include spontaneous alternation. We have thus tested spatial working memory in dopamine transporter knockout (DAT KO) and wild-type mice. Spontaneous alternation in the Y-maze, an index of short-term spatial working memory in mice, was significantly decre... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3027218 Sat, 21 Nov 2009 00:00:00 +0100 3027218 http://www.medworm.com/index.php?rid=3027219&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19932695%26dopt%3DAbstract Authors: Dai X, Song HJ, Cui SG, Wang T, Liu Q, Wang R The opioid peptides modulate extensive bioactivities, including pain, cardiovascular response, development and further responses. In the present study, the stimulative effects of endogenous opioid peptides on angiogenesis are evaluated in the proliferation, migration, adhesion and tube formation assays of the human umbilical vein endothelial cell (HUVEC) for the first time. Endomorphin-1, endomorphin-2 and deltorphin I at physiological concentrations could stimulate HUVECs proliferation, migration, adhesion and tube formation in a dose dependent manner; whereas, they exhibited the cytotoxic effects on HUVECs at the higher doses in these assays. Naloxone, the nonselective opioid receptor antagonist, did not influence angiogenesis wh... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3027219 Fri, 20 Nov 2009 00:00:00 +0100 3027219 http://www.medworm.com/index.php?rid=3027220&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19932093%26dopt%3DAbstract Authors: Catlow BJ, Badanich KA, Sponaugle AE, Rowe AR, Song S, Rafalovich I, Sava V, Kirstein CL, Sanchez-Ramos J The use of 3,4,methylenedioxymethamphetamine (MDMA), the active agent in ecstasy, during adolescence is widespread yet the effects on adolescent behavior and brain development are unknown. The aim of the present study was 1) to evaluate effects of MDMA in adolescent rats using the conditioned place preference (CPP) paradigm to measure MDMA-induced reward and 2) assess effects of MDMA administration on cellular proliferation, survival and neurogenesis in the dentate gyrus of the hippocampus. During the adolescent period, MDMA CPP was measured in adolescents [postnatal day (PND) 28-39] by training rats to associate 1.25, 2.5, 5.0mg/kg MDMA or saline administration with envir... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3027220 Thu, 19 Nov 2009 00:00:00 +0100 3027220 http://www.medworm.com/index.php?rid=3027221&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19931526%26dopt%3DAbstract In conclusion, the results suggested that rutin (50microM) blocked apoptosis in HUVECs through decreasing reactive oxygen species, increasing GSH, restoring Deltapsim and thus protecting DNA damage. Our research indicated that rutin protected the intracellular GSH antioxidant system and prevented H(2)O(2)-induced apoptosis of HUVECs through regulating reactive oxygen species mediated mitochondrial dysfunction pathway. PMID: 19931526 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3027221 Wed, 18 Nov 2009 00:00:00 +0100 3027221 http://www.medworm.com/index.php?rid=3027222&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19931239%26dopt%3DAbstract In conclusion, both m-3M3FBS and o-3M3FBS inhibit inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, both compounds also caused an increase in [Ca(2+)](i) in an agonistic manner. Therefore caution must be employed when interpreting their effects at the tissue and cellular level. PMID: 19931239 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3027222 Tue, 17 Nov 2009 00:00:00 +0100 3027222 http://www.medworm.com/index.php?rid=3017257&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19925785%26dopt%3DAbstract In conclusion, formoterol and ipratropium bromide partially protect the lungs against the inflammation by reducing neutrophilic infiltration. This protective effect is associated with reduced MMP-9 activity known to play an important pro-inflammatory role in acute inflammatory process. PMID: 19925785 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3017257 Mon, 16 Nov 2009 00:00:00 +0100 3017257 http://www.medworm.com/index.php?rid=3017256&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19925786%26dopt%3DAbstract Authors: Schmid D, Staudacher DL, Plass CA, Loew HG, Fritz E, Steurer G, Chiba P, Moeslinger T We tested the hypothesis, that ATP-sensitive potassium (K(ATP)) channels limit cardiac energy demand by a feedback control of mean power output at increased cardiac rates. We analysed the interrelationships between rising energy demand of adult rat and guinea pig left ventricular papillary muscle and down-regulatory electromechanical effects mediated by K(ATP)-channels. Using the K(ATP)-opener pinacidil the stimulation frequency was increased stepwise and mechanical parameters and action potentials were recorded. Power output was derived from force-length area or force-time integral calculations, respectively. Simultaneously oxygen availability in the preparations was estimated by flavoprotei... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3017256 Mon, 16 Nov 2009 00:00:00 +0100 3017256 http://www.medworm.com/index.php?rid=3017255&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19925787%26dopt%3DAbstract Authors: Leppänen T, Jalonen U, Korhonen R, Tuominen RK, Moilanen E Tristetraprolin (TTP) binds to AU-rich elements within the mRNAs of several inflammatory genes and causes destabilization of the target mRNAs. The protein kinase C (PKC) pathway represents a major signalling system in inflammation and PKCdelta is one of the key isoenzymes in the regulation of inflammatory processes. In the present study, we investigated the role of PKCdelta in the regulation of the expression of tristetraprolin in activated macrophages by using the PKCdelta inhibitor, rottlerin, and by downregulating PKCdelta expression by using PKCdelta siRNA. TTP protein and mRNA expression were measured by Western blotting and quantitative RT-PCR, respectively. TTP and TNFalpha mRNA decays were studied by the a... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3017255 Mon, 16 Nov 2009 00:00:00 +0100 3017255 http://www.medworm.com/index.php?rid=3013084&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19919831%26dopt%3DAbstract Authors: Tsubosaka Y, Murata T, Kinoshita K, Yamada K, Uemura D, Hori M, Ozaki H Halichlorine, isolated from a marine sponge Halichondria okadai Kadota, has an unique structure and it's physiological activity virtually unknown. In the present study, we investigated the direct effect of halichlorine on vascular contractility. In endothelium-denuded rat aorta, while the treatment of halichlorine (0.01-10muM) didn't induce vascular contraction, halichlorine (0.01-10muM) dose-dependently inhibited both the steady state precontractions induced by high K(+) (65.4mM) and phenylephrine (1muM). The vasodilator effect of halichlorine (10muM) on high K(+) (65.4mM)-induced contraction was more potent than that on phenylephrine (1muM)-induced contraction (65.4mM high K(+): 72.7+/-3.4%; 1muM phenyle... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3013084 Sat, 14 Nov 2009 00:00:00 +0100 3013084 http://www.medworm.com/index.php?rid=3013083&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19919832%26dopt%3DAbstract Authors: Song GM, Huan Y, Sun SJ, Chen YT, Liu Q, Shen ZF Exendin-4 is an incretin mimetic that has been developed for the treatment of patients with type 2 diabetes. And EXf is an available carboxy-terminal truncated fragment of exendin-4 with two amino acid substitutions. The purpose of these studies was to evaluate the biological activity of EXf. After a single subcutaneous injection, EXf significantly decreased plasma glucose concentration and glucose excursion following the administration of an oral glucose challenge both in non-diabetic (ICR), monosodium L-glutamate induced insulin resistance (MSG-IR) and diabetic KK-ay mice. Meanwhile, EXf resulted in an increase of first-phase insulin secretion in normal mice and KK-ay mice following the glucose challenge. EXf was also shown to... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3013083 Sat, 14 Nov 2009 00:00:00 +0100 3013083 http://www.medworm.com/index.php?rid=3013082&cid=s_35551_13_f&fid=35551&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D19919833%26dopt%3DAbstract Authors: Dhaese I, Van Colen I, Lefebvre RA Hydrogen sulfide (H(2)S) has been suggested as a gaseous neuromodulator in mammals. The aim of this study was to examine the influence of H(2)S on contractility in mouse distal colon. The effect of sodium hydrogen sulfide (NaHS; H(2)S donor) on prostaglandin F(2alpha) (PGF(2alpha))-contracted circular muscle strips of mouse distal colon was investigated. In addition, tension and cytosolic calcium concentration ([Ca(2+)](cyt)) in the mouse distal colon strips were measured simultaneously in the presence of NaHS. NaHS caused concentration-dependent relaxation of the pre-contracted mouse distal colon strips. The NaHS-induced relaxation was not influenced by the K(+) channels blockers glibenclamide, apamin, charybdotoxin, barium chloride and 4-am... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=3013082 Sat, 14 Nov 2009 00:00:00 +0100 3013082