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. Wed, 08 Feb 2012 14:04:15 +0100 http://www.medworm.com/index.php?rid=5643876&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%3D22285855%26dopt%3DAbstract In conclusion, the enhancement of vasopressin V1b receptor-mediated ACTH release and the lack of a detectable vasopressin V1b receptor coupling to [Ca(2+)]i increase in cultured cells suggests the activation of a different/additional signaling pathway in the molecular mechanism of ACTH release. PMID: 22285855 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5643876 Fri, 20 Jan 2012 05:00:00 +0100 5643876 http://www.medworm.com/index.php?rid=5626230&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%3D22265725%26dopt%3DAbstract We examined the effects of angiotensin AT(1) receptor blockers on the formation of foam cells from macrophages. When macrophages from a human cell line were stimulated with oxidized low-density lipoprotein (oxLDL), the angiotensin AT(1) receptor blockers candesartan and losartan attenuated the intracellular accumulation of cholesterol ester and the increases in mRNA and protein levels of ACAT-1. Moreover, the increase in oxLDL-induced ACAT-1 was reduced by AG1478, an inhibitor of the epidermal growth factor (EGF) receptor. Additionally, oxLDL up-regulated the protein level of heparin-binding EGF-like growth factor (HB-EGF), a ligand of the EGF receptor. Inhibitors of angiotensin-converting enzyme affected neither cholesterol ester accumulation nor the expression of ACAT-1. Although oxLDL i... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5626230 Mon, 16 Jan 2012 05:00:00 +0100 5626230 http://www.medworm.com/index.php?rid=5626225&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%3D22269225%26dopt%3DAbstract We examined the effects of ethanol on the phosphorylation of CREB in hepatocytes, and in vivo in rat liver after chronic ethanol binge. For in vivo studies, rats were fed ethanol in liquid diet for 4weeks followed by single binge administration of ethanol (intragastric, 5g/kg body weight). Four hours after binge administration, liver samples were collected and analyzed. Treatment of hepatocytes with ethanol caused increased phosphorylation of p38 MAPK (mitogen activated protein kinase), MSK-1 (mitogen and stress activated kinase) and CREB in the nuclear compartment without activation of ERK1/2 (extracellular regulated kinase); whereas angiotensin II induced activation of CREB was accompanied by activation of ERK1/2. In chronic ethanol-binge studies, analysis of the whole cell extracts show... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5626225 Sun, 15 Jan 2012 05:00:00 +0100 5626225 http://www.medworm.com/index.php?rid=5626229&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%3D22265864%26dopt%3DAbstract Authors: Ribeiro A, Ferraz-de-Paula V, Pinheiro ML, Vitoretti LB, Mariano-Souza DP, Quinteiro-Filho WM, Akamine AT, Almeida VI, Quevedo J, Dal-Pizzol F, Hallak JE, Zuardi AW, Crippa JA, Palermo-Neto J Abstract Acute lung injury is an inflammatory condition for which treatment is mainly supportive because effective therapies have not been developed. Cannabidiol, a non-psychotropic cannabinoid component of marijuana (Cannabis sativa), has potent immunosuppressive and anti-inflammatory properties. Therefore, we investigated the possible anti-inflammatory effect of cannabidiol in a murine model of acute lung injury. Analysis of total inflammatory cells and differential in bronchoalveolar lavage fluid was used to characterize leukocyte migration into the lungs; myeloperoxidase activity ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5626229 Thu, 12 Jan 2012 05:00:00 +0100 5626229 http://www.medworm.com/index.php?rid=5626228&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%3D22266490%26dopt%3DAbstract Authors: Silambarasan T, Raja B Abstract The present study was aimed to evaluate the antihypertensive effect of diosmin in deoxycorticosterone acetate (DOCA)-salt induced hypertension in male Wistar rats. Hypertension was induced in uninephrectomized rats by weekly twice subcutaneous injection of DOCA (25mg/kg body weight) and 1% NaCl in the drinking water for six consecutive weeks. The important pathological events that occurred in DOCA-salt treated rats were significant increase in systolic, diastolic blood pressure, sodium and chloride in serum and lipid peroxidation products (thiobarbituric acid reactive substances, lipid hydroperoxides and conjugated dienes) in plasma and tissues (liver, kidney, heart and aorta) and significant decrease in serum potassium, total nitrite and ni... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5626228 Thu, 12 Jan 2012 05:00:00 +0100 5626228 http://www.medworm.com/index.php?rid=5626227&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%3D22266491%26dopt%3DAbstract This study was performed to explore whether the cardioprotective effect of alpha lipoic acid was related to activation of ALDH2 and the underlying mechanisms. In a Langendorff model of ischemia-reperfusion in rats, cardiac function, activities of creatine kinase (CK) and ALDH2, contents of 4-hydroxy-2-nonenal (4-HNE) and malondialdehyde (MDA) were measured. In a cell model of hypoxia-reoxygenation, the apoptosis, ALDH activity, reactive oxygen species level, 4-HNE and MDA contents were examined. In the isolated hearts, ischemia-reperfusion treatment led to cardiac dysfunction accompanied by an increase in 4-HNE and MDA contents. Pretreatment with lipoic acid significantly up-regulated myocardial ALDH2 activity concomitantly with an improvement of cardiac dysfunction and a decrease in 4-HNE... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5626227 Thu, 12 Jan 2012 05:00:00 +0100 5626227 http://www.medworm.com/index.php?rid=5626226&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%3D22266492%26dopt%3DAbstract In this study, we aimed to verify the possible antidepressant-like effect of acute oral administration of ferulic acid in the forced swimming test (FST) and tail suspension test (TST) in mice. Additionally, the mechanisms involved in the antidepressant-like action and the effects of the association of ferulic acid with the antidepressants fluoxetine, paroxetine, and sertraline in the TST were investigated. Ferulic acid produced an antidepressant-like effect in the FST and TST (0.01-10mg/kg, p.o.), without accompanying changes in ambulation. The pretreatment of mice with WAY100635 (0.1mg/kg, s.c., a selective 5-HT(1A) receptor antagonist) or ketanserin (5mg/kg, i.p., a 5-HT(2A) receptor antagonist) was able to reverse the anti-immobility effect of ferulic acid (0.01mg/kg, p.o.) in the TST. ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5626226 Thu, 12 Jan 2012 05:00:00 +0100 5626226 http://www.medworm.com/index.php?rid=5580123&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%3D22222823%26dopt%3DAbstract This study was designed to confirm this cardiac protection by use of a dog CPB model and to elucidate the related mechanism. Adult mongrel male dogs undergoing standard CPB were assigned into 4 groups: Sham group, Propofol group, Isoflurane (Iso) group and isoflurane in combination of propofol (pre-Iso+P) group. After induction, anesthesia was maintained with propofol (Propofol group), isoflurane (Iso group) or isoflurane preconditioning in combination with propofol posttreatment (pre-Iso+P group). After 2h cardiac arrest and CPB, aortic cross-clamping was released to allow 2h reperfusion. The results demonstrated that joint use of isoflurane and propofol facilitated cardiac functional recovery, improved myocardial oxygen utilization and decreased cardiac enzyme release. Also, the oxidativ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580123 Thu, 29 Dec 2011 05:00:00 +0100 5580123 http://www.medworm.com/index.php?rid=5580121&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%3D22227330%26dopt%3DAbstract In this report we studied the effects of neferine, a major alkaloid component in lotus embryos, on human osteosarcoma cells and the underlying mechanisms. We found that neferine possessed a potent growth-inhibitory effect on human osteosarcoma cells, but not on non-neoplastic human osteoblast cells. The inhibitory effect of neferine on human osteosarcoma cells was largely attributed to cell cycle arrest at G1. The induction of G1 arrest was p21(WAF1/CIP1)-dependent, but was independent of p53 or RB (retinoblastoma-associated protein). The up-regulation of p21 by neferine was due to an increase in the half-life of p21 protein. We examined four kinases that are known to affect the stabilization of p21, and found that p38 MAPK and JNK were activated by neferine. However, only SB203580 (an inh... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580121 Thu, 29 Dec 2011 05:00:00 +0100 5580121 http://www.medworm.com/index.php?rid=5580120&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%3D22227331%26dopt%3DAbstract Authors: Miszkiel J, Adamczyk P, Filip M, Przegaliński E Abstract A number of data indicate that serotonin (5-HT) 5-HT(1B) receptor ligands affect the behavioral effects of psychostimulants. In the present study we examined effects of the selective 5-HT(1B) receptor antagonist N-[3-[3-(dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride (SB 216641) and the agonist 5-propoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-pyrrolo[3,2-b]pyridine hydrochloride (CP 94253) on amphetamine self-administration in rats. SB 216641 administered in doses of 2.5-7.5mg/kg did not affect the self-administration of amphetamine injected in unit doses of 0.06 or 0.12mg/kg/infusion. On the other hand, CP 94253 administered in doses of... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580120 Thu, 29 Dec 2011 05:00:00 +0100 5580120 http://www.medworm.com/index.php?rid=5580119&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%3D22227332%26dopt%3DAbstract In this study, the programmed cell death and autophagy induced by two nitrostyrene derivative compounds (NTS1 and NTS2) was studied using the tumorigenic Ehrlich ascitic tumor (EAT) cells. EAT cells were highly sensitive to NTS1 and NTS2 cytotoxicity in a dose-dependent manner. NTS1 and NTS2 IC(50) was less than 15.0μM post 12h incubation. Apoptosis was primarily induced by both compounds, as demonstrated by an increase in Annexin-V positive cells, concurrently with cytochrome c release from mitochondria to cytosol and caspase-3 activation. Although cytosolic Ca(2+) mobilization is involved in autophagy as well as apoptosis in response to cellular stress in many cancer cell types, from the two nitrostyrene derivative compounds studied, mainly NTS1 mobilized this ion and disparate autophag... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580119 Thu, 29 Dec 2011 05:00:00 +0100 5580119 http://www.medworm.com/index.php?rid=5580118&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%3D22227333%26dopt%3DAbstract In this study, targeting the liver as one of the organs that plays an important role in energy metabolism, Flavangenol was investigated for its effect on non-alcoholic fatty liver disease (NAFLD), its action mechanism and its active ingredients, using in vivo and in vitro experiment systems. Flavangenol suppressed intrahepatic fat accumulation in Western diet-loaded Tsumura Suzuki Obese Diabetes (TSOD) mice, which develop various metabolic diseases. In addition, Flavangenol significantly increased the mRNA expression levels of fatty acid oxidative enzymes (peroxisomal proliferator-activated receptor α, acyl-CoA oxidase, carnitine palmitoyltransferase). In order to investigate the direct effect of Flavangenol on the liver, an in vitro fatty liver model prepared by adding a free fatty acid ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580118 Thu, 29 Dec 2011 05:00:00 +0100 5580118 http://www.medworm.com/index.php?rid=5580117&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%3D22227334%26dopt%3DAbstract This study provides the first evidence that genistein has neuroprotective effects against 6-OHDA-induced neurotoxicity in SK-N-SH cells and activation of the IGF-I receptor signaling pathway might be involved in actions of genistein. PMID: 22227334 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580117 Thu, 29 Dec 2011 05:00:00 +0100 5580117 http://www.medworm.com/index.php?rid=5580116&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%3D22227335%26dopt%3DAbstract Authors: Pernomian L, Gomes MS, Restini CB, Ramalho LN, Tirapelli CR, de Oliveira AM Abstract The modulation played by reactive oxygen species on the angiotensin II-induced contraction in type I-diabetic rat carotid was investigated. Concentration-response curves for angiotensin II were obtained in endothelium-intact or endothelium-denuded carotid from control or streptozotocin-induced diabetic rats, pre-treated with tiron (superoxide scavenger), PEG-catalase (hydrogen peroxide scavenger), dimethylthiourea (hydroxyl scavenger), apocynin [NAD(P)H oxidase inhibitor], SC560 (cyclooxygenase-1 inhibitor), SC236 (cyclooxygenase-2 inhibitor) or Y-27632 (Rho-kinase inhibitor). Reactive oxygen species were measured by flow cytometry in dihydroethidium (DHE)-loaded endothelial cells. Cycloox... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580116 Thu, 29 Dec 2011 05:00:00 +0100 5580116 http://www.medworm.com/index.php?rid=5580115&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%3D22227336%26dopt%3DAbstract Authors: Yin CY, Yeen LS, Ha TS, Kadir KB Abstract The activities of phosphoenolpyruvate carboxykinase (PEPCK) are influenced by active glucocorticoids which are activated by 11-β-hydroxysteroid dehydrogenase 1 (11β-HSD1) while hexose-6-phosphate dehydrogenase (H6PDH) influences the activities of 11-βHSD1 in a cofactor manner. Dysregulation of PEPCK and H6PDH has been associated with the pathogenesis of metabolic syndrome. Sixteen male Sprague Dawley rats, fed ad libitum, were assigned to two groups, control and treated, with the treated group being given GA at 100mg/kg for one week. Blood and subcutaneous and visceral adipose tissue, abdominal and quadriceps femoris muscle, liver and kidney were examined. GA treatment led to an overall significant decrease in blood glucose whil... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580115 Thu, 29 Dec 2011 05:00:00 +0100 5580115 http://www.medworm.com/index.php?rid=5580114&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%3D22227337%26dopt%3DAbstract Authors: González LG, Sánchez-Fernández C, Cobos EJ, Baeyens JM, Del Pozo E Abstract Several lines of evidence suggest that σ(1) receptors regulate intracellular calcium concentration [Ca(2+)](i). However, no previous studies have demonstrated a consistent role for these receptors in the modulation of extracellular calcium entry through plasmalemmal voltage-dependent calcium channels (VDCCs). To search for evidence of such a role we compared [Ca(2+)](i) under basal conditions and after depolarization with KCl in fura-2-loaded synaptosomes from wild-type and σ(1) receptor knockout (σ(1)R-KO) mice. We also tested the effects of the selective σ(1) receptor agonists PRE-084 and (+)-pentazocine and antagonists BD-1047 and NE-100 on the increase in [Ca(2+)](i) induced by depolariz... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580114 Thu, 29 Dec 2011 05:00:00 +0100 5580114 http://www.medworm.com/index.php?rid=5580113&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%3D22227379%26dopt%3DAbstract Authors: Soliman M, Arafah M Abstract Hemorrhagic shock is a leading cause of death despite the improvement in emergency services. One reason is that the resuscitation policies are designed to reestablish tissue perfusion, but not to prevent the inflammatory response to shock that cause myocardial dysfunction and injury. Dipyridamole is a platelet inhibitor that promotes anti-inflammatory effects. The present study investigated the therapeutic value of treatment with dipyridamole before resuscitation from hemorrhagic shock on myocardial injury and protection. Male Sprague-Dawley rats were assigned to 3 experimental groups (n=6 per group): 1) hemorrhage, 2) hemorrhage treated with dipyridamole, and 3) sham hemorrhage. Rats were hemorrhaged over 60min to reach a mean arterial blood p... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580113 Thu, 29 Dec 2011 05:00:00 +0100 5580113 http://www.medworm.com/index.php?rid=5580127&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%3D22222819%26dopt%3DAbstract Authors: Shim HS, Ok SH, Lee SH, Kwon SC, Sohn JT Abstract Levobupivacaine is a long-acting amide local anesthetic that intrinsically produces vasoconstriction both in vivo and in vitro. Levobupivacaine increases intracellular calcium concentrations ([Ca(2+)](i)) in vascular smooth muscle cells. The goals of this in vitro study were to investigate whether levobupivacaine-induced contraction is associated with increased Ca(2+) sensitivity and to identify the protein kinases involved in mediating contraction in response to levobupivacaine in isolated rat aortic smooth muscle. The effect of levobupivacaine and potassium chloride (KCl) on the [Ca(2+)](i) and tension was measured simultaneously with acetoxymethyl ester of fura-2-loaded aortic strips. Cumulative levobupivacaine concentra... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580127 Tue, 27 Dec 2011 05:00:00 +0100 5580127 http://www.medworm.com/index.php?rid=5580126&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%3D22222820%26dopt%3DAbstract Authors: Inoue M, Ishibashi Y, Nogawa H, Yasue T Abstract Clearance of apoptotic cells, so-called efferocytosis, by alveolar macrophages (AMs) is important for lung homeostasis and is impaired in pulmonary inflammatory diseases, such as chronic obstructive pulmonary disease and asthma. Carbocisteine, a mucoregulatory drug, corrects the contents of fucose in airway mucus and has anti-inflammatory properties in airway inflammation. Thus, we conducted the present study to better understand the anti-inflammatory properties of carbocisteine. First, we induced airway inflammation in mice with lipopolysaccharide intratracheally. Carbocisteine significantly decreased neutrophil numbers in bronchoalveolar lavage fluid at the resolution phase of inflammation, implying the promotion of neutro... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580126 Tue, 27 Dec 2011 05:00:00 +0100 5580126 http://www.medworm.com/index.php?rid=5580125&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%3D22222821%26dopt%3DAbstract In conclusion, pirfenidone is capable of impairing Th2 differentiation and limits Th2 profibrogenic response. The mechanism involves p38 inhibition and regulation of GATA3 expression and translocation. PMID: 22222821 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580125 Tue, 27 Dec 2011 05:00:00 +0100 5580125 http://www.medworm.com/index.php?rid=5580124&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%3D22222822%26dopt%3DAbstract In conclusion, this study indicates that LPS-induced oxidative stress leads to functional damages in the testicular mitochondria. Lycopene pretreatment provided a marked normalization in these parameters. PMID: 22222822 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580124 Tue, 27 Dec 2011 05:00:00 +0100 5580124 http://www.medworm.com/index.php?rid=5580122&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%3D22227329%26dopt%3DAbstract This study presents columbin as a potential anti-inflammatory drug. PMID: 22227329 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5580122 Tue, 27 Dec 2011 05:00:00 +0100 5580122 http://www.medworm.com/index.php?rid=5567266&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%3D22214536%26dopt%3DAbstract In conclusion, trachylobane-360 and trachylobane-318 induced spasmolytic activity by K(+) channel positive modulation and Ca(2+) channel blockade, which results in [Ca(2+)](c) reduction at cellular level leading to smooth muscle relaxation. PMID: 22214536 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567266 Tue, 27 Dec 2011 05:00:00 +0100 5567266 http://www.medworm.com/index.php?rid=5567270&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%3D22209879%26dopt%3DAbstract In conclusion, the new thienopyridine analogs were promising for the potential use as anti-inflammatory agents for both acute and chronic inflammatory disorders with low toxic effects. PMID: 22209879 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567270 Sat, 24 Dec 2011 05:00:00 +0100 5567270 http://www.medworm.com/index.php?rid=5567273&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%3D22209876%26dopt%3DAbstract Authors: Li F, Liu S, Ouyang Y, Fan C, Wang T, Zhang C, Zeng B, Chai Y, Wang X Abstract In the present study, the effects of celecoxib on proliferation, collagen expression, ERK1/2 and SMAD2/3 phosphorylation in NIH/3T3 fibroblasts were investigated. NIH/3T3 fibroblasts stimulated with fibroblast growth factor-2 (FGF-2) or transforming growth factor-β1 (TGF-β1) were examined in the presence of celecoxib. Proliferation was assessed by MTT assays; ERK1/2 expression and SMAD2/3 expression were assessed by quantitative RT-PCR and western blotting; ERK1/2 phosphorylation and SMAD2/3 phosphorylation were assessed by western blot analysis. The results indicated that celecoxib could suppress cell proliferation stimulated by FGF-2 (IC(50) FGF+group, 75±1.9μmol/l) and TGF-β1 (IC(50) TGF... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567273 Fri, 23 Dec 2011 05:00:00 +0100 5567273 http://www.medworm.com/index.php?rid=5567272&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%3D22209877%26dopt%3DAbstract Authors: Nujić K, Smith M, Lee M, Belamarić D, Tomašković L, Alihodžić S, Malnar I, Polančec D, Schneider K, Haber VE Abstract In addition to antibacterial activity, some macrolide antibiotics, such as azithromycin and clarithromycin, also exhibit anti-inflammatory properties in vitro and in vivo, although the targets and mechanism(s) of action remain unknown. The aim of the present study was to identify protein targets of azithromycin and clarithromycin which could potentially explain their anti-inflammatory effects. Using chemical proteomics approach, based on compound-immobilized affinity chromatography, valosin containing protein (VCP) was identified as a potential target of the macrolides. Validation studies confirmed the interaction of macrolides and VCP and gave some ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567272 Fri, 23 Dec 2011 05:00:00 +0100 5567272 http://www.medworm.com/index.php?rid=5567271&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%3D22209878%26dopt%3DAbstract In conclusion, multiple airway antigen challenges induced the proliferation of IL-10-expressing CD4(±) T cells in regulating airway neutrophilia. Systemic blockade of IL-10 function coincided with increases in IL-1β and CXC chemokines. Thus, IL-1β and CXC chemokines may be targets for development of novel pharmacotherapy for neutrophilic asthma. PMID: 22209878 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567271 Fri, 23 Dec 2011 05:00:00 +0100 5567271 http://www.medworm.com/index.php?rid=5567269&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%3D22209880%26dopt%3DAbstract This study was aimed to assess the ketamine's differential effect on water maze memory acquisition, consolidation and retrieval. Male Sprague-Dawley rats (250-350g) were trained in water maze single training session. 24h later a probe trial which was consisted of a single trial without platform was done. To assess the effect of ketamine on water maze memory acquisition it was administered before training; to assess its effect on memory consolidation it was administered immediately after training and to assess its effect on memory retrieval it was injected before probe trial. Ketamine both in sub-anesthetic and anesthetic doses impaired water maze memory acquisition, its anesthetic dose but not sub-anesthetic dose impaired memory consolidation and on retrieval stage, both doses deteriorated... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567269 Fri, 23 Dec 2011 05:00:00 +0100 5567269 http://www.medworm.com/index.php?rid=5567268&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%3D22209881%26dopt%3DAbstract Authors: Kim H, Bang J, Chang HW, Kim JY, Park KU, Kim SH, Lee KJ, Cho CH, Hwang I, Park SD, Ha E, Jung SW Abstract Quetiapine is an atypical antipsychotic and has also been used in the treatment of depression. Since anti-inflammatory effects of antidepressants are well established, we hypothesized that quetiapine may also exert anti-inflammatory effects. Thus this study was designed to examine the anti-inflammatory effect of quetiapine in murine collagen-induced arthritis. Mice were immunized with collagen type II for the induction of arthritis and treated with quetiapine (10mg/kg) daily for 2weeks. Mice were divided into 3 groups: control, CIA, and CIA+quetiapine treatment. Arthritic index and paw thickness were used to compare severity of arthritis. In additions, radiological an... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567268 Fri, 23 Dec 2011 05:00:00 +0100 5567268 http://www.medworm.com/index.php?rid=5567276&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%3D22206815%26dopt%3DAbstract In conclusion, the present data substantiate antidepressive effects of pramipexole and indicate a contribution of the dopaminergic and serotonergic metabolism in these effects, but argue against an eminent role of BDNF. PMID: 22206815 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567276 Thu, 22 Dec 2011 05:00:00 +0100 5567276 http://www.medworm.com/index.php?rid=5567275&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%3D22206816%26dopt%3DAbstract Authors: Yoshizumi M, Eisenach JC, Hayashida KI Abstract We have recently demonstrated that the glutamate transporter activator riluzole paradoxically enhanced glutamate-induced glutamate release from cultured astrocytes. We further showed that both riluzole and the α(2)δ subunit ligand gabapentin activated descending inhibition in rats by increasing glutamate receptor signaling in the locus coeruleus and hypothesized that these drugs share common mechanisms to enhance glutamate release from astrocytes. In the present study, we examined the effects of riluzole and gabapentin on glutamate uptake and release and glutamate-induced Ca(2+) responses in primary cultures of astrocytes. Riluzole and gabapentin facilitated glutamate-induced glutamate release from astrocytes and significan... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567275 Wed, 21 Dec 2011 05:00:00 +0100 5567275 http://www.medworm.com/index.php?rid=5567274&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%3D22206817%26dopt%3DAbstract In this study, we investigated the role of descending serotonergic pathways and spinal 5-HT(7) receptors compared with 5-HT(3) and 5-HT(2A) receptors in the antinociceptive and antihyperalgesic effects of paracetamol. Tail-flick, hot plate and plantar incision tests were used to determine nociception in male BALB/c mice. Lesion of serotonergic bulbospinal pathways was performed by intrathecal (i.th.) injection of 5,7-dihydroxytryptamine (5,7-DHT), and spinal 5-HT levels were measured by HPLC. To evaluate the particular subtypes of the spinal 5-HT receptors, the selective 5-HT(7), 5-HT(3) and 5-HT(2A) receptor antagonists SB 269970, ondansetron and ketanserin, respectively, were given i.th. after oral administration of paracetamol. Oral paracetamol (200, 400 and 600mg/kg) elicits dose-depen... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567274 Wed, 21 Dec 2011 05:00:00 +0100 5567274 http://www.medworm.com/index.php?rid=5567267&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%3D22210053%26dopt%3DAbstract Authors: Bonaventura MM, Crivello M, Ferreyra ML, Repetto M, Cymeryng C, Libertun C, Lux-Lantos VA Abstract γ-Aminobutyric acid (GABA) inhibits insulin secretion through GABA(B) receptors in pancreatic β-cells. We investigated whether GABA(B) receptors participated in the regulation of glucose homeostasis in vivo. BALB/c mice acutely pre-injected with the GABA(B) receptor agonist baclofen (7.5mg/kg, i.p.) presented glucose intolerance and diminished insulin secretion during a glucose tolerance test (GTT, 2g/kg body weight, i.p.). The GABA(B) receptor antagonist 2-hydroxysaclofen (15mg/kg, i.p.) improved the GTT and reversed the baclofen effect. Also a slight increase in insulin secretion was observed with 2-hydroxysaclofen. In incubated islets 1.10(-5)M baclofen inhibited 20mM gl... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5567267 Wed, 21 Dec 2011 05:00:00 +0100 5567267 http://www.medworm.com/index.php?rid=5552444&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%3D22200628%26dopt%3DAbstract Authors: Lee JS, Kang Y, Kim JT, Thapa D, Lee ES, Kim JA Abstract Abnormal angiogenesis plays a critical role in the pathogenesis of various diseases such as cancer and chronic inflammation. A variety of pro-angiogenic factors, including vascular endothelial growth factor (VEGF), exert their action through endothelial receptor tyrosine kinases (RTKs). The synthetic phenylpropenone derivatives, used in this study were the following: 1,3-diphenyl-propenone (DPhP), 3-phenyl-1-thiophen-2-yl-propenone (PhT2P), 3-phenyl-1-thiophen-3-yl-propenone (PhT3P) and 1-furan-2-yl-3-phenyl-propenone (FPhP). These derivatives were screened for their inhibitory effect on VEGF-induced angiogenesis in vitro using HUVECs and in vivo using chick chorioallantoic membrane (CAM). The order of anti-angiogeni... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552444 Tue, 20 Dec 2011 05:00:00 +0100 5552444 http://www.medworm.com/index.php?rid=5552440&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%3D22202844%26dopt%3DAbstract Authors: Devavry S, Legros C, Brasseur C, Cohen W, Guenin SP, Delagrange P, Malpaux B, Ouvry C, Cogé F, Nosjean O, Boutin JA Abstract The main melatonin receptors are two G-protein coupled receptors named MT(1) and MT(2). Having described the molecular pharmacology of the human versions of these receptors, we turned to two of the three species most useful in studying melatonin physiology: rat and sheep (a diurnal species used to understand the relationship between circadian rhythm and depression). We also employed previously used compounds to describe the mouse melatonin receptors; despite the early cloning of mouse receptors, few molecular pharmacology studies on these receptors exist. To our surprise, we detected no major differences between the data obtained from mice and those... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552440 Tue, 20 Dec 2011 05:00:00 +0100 5552440 http://www.medworm.com/index.php?rid=5552441&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%3D22200631%26dopt%3DAbstract In conclusion, TP receptor stimulation is suggested to be coupled with PC-PLC. Diacylglycerol produced by PC-PLC seems to activate two types of cation channels independently of PKC, which in turn leads to VDCC-dependent and independent Ca(2+) influx, thereby eliciting contraction. PMID: 22200631 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552441 Mon, 19 Dec 2011 05:00:00 +0100 5552441 http://www.medworm.com/index.php?rid=5552449&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%3D22197649%26dopt%3DAbstract In this study, we tested the effects of Ginkgolide B (GB) and bilobalide (BB) on normoglycemic and hyperglycemic rats subjected to transient cerebral ischemia. Rats were administered p.o. with different Ginkgo components GB (6mg/kg) or BB (6mg/kg) once daily for 7days. Hyperglycemia was made by jugular vein infusion of glucose and transient middle cerebral artery occlusion/reperfusion was induced by a suture insertion technique. Results showed that both GB and BB exerted neuroprotection under normoglycemia, as determined by infarct volume and neurological deficit scores. Yet, BB showed less protective effects during hyperglycemic cerebral ischemia. Cerebral blood flow (CBF) was evaluated during occlusion and the first hour of reperfusion. BB but not GB caused acute increase in CBF after re... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552449 Fri, 16 Dec 2011 05:00:00 +0100 5552449 http://www.medworm.com/index.php?rid=5552447&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%3D22200625%26dopt%3DAbstract Authors: An L, Liu CT, Yu MJ, Chen ZH, Guo XG, Peng-Wang , Wang JF, Fang XQ, Gao YH, Yu SY Abstract Mechanical ventilation is an indispensable supportive intervention for acute respiratory failure. However, mechanical ventilation can provoke ventilator-induced lung injury, which remains one of the major causes of morbidity and mortality in critically ill patients. Excessive inflammatory response characterized by infiltration of inflammatory cells and overproduction of inflammatory mediators contributes to the pathogenesis of ventilator-induced lung injury. At present, apart from the protective ventilation strategy, no other pharmacological intervention is available to attenuate ventilator-induced lung injury. Heme oxygenase-1 (HO-1) is the inducible isoform of the first and rate-li... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552447 Fri, 16 Dec 2011 05:00:00 +0100 5552447 http://www.medworm.com/index.php?rid=5552446&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%3D22200626%26dopt%3DAbstract In this study, we explored the possibility that adenosine A(1) and TPα receptors form hetero-oligomers with novel pharmacological profiles. We showed that these receptors hetero-oligomerize by conducting coimmunoprecipitation and bioluminescence resonance energy transfer (BRET(2)) assays in adenosine A(1) receptor and TPα receptor-cotransfected HEK293T cells. Furthermore, coexpression of the receptors affected signal transduction including the accumulation of cyclic AMP and phosphorylation of extracellular signal-regulated kinase-1 and -2 was significantly increased by high and low concentrations of adenosine A(1) receptor agonist and TPα agonists, respectively. Our study provides evidence of hetero-oligomerization between adenosine A(1) and TPα receptors for the first time, and sugges... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552446 Fri, 16 Dec 2011 05:00:00 +0100 5552446 http://www.medworm.com/index.php?rid=5552445&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%3D22200627%26dopt%3DAbstract Authors: Ondrejcak T, Wang Q, Kew JN, Virley DJ, Upton N, Anwyl R, Rowan MJ Abstract Nicotinic acetylcholine receptors mediate fast cholinergic modulation of glutamatergic transmission and synaptic plasticity. Here we investigated the effects of subtype selective activation of the α7 nicotinic acetylcholine receptors on hippocampal transmission and the inhibition of synaptic long-term potentiation by the Alzheimer's disease associated amyloid ß-protein (Aß). The α7 nicotinic acetylcholine receptor agonist "compound A" ((R)-N-(1-azabicyclo[2.2.2]oct-3-yl)(5-(2-pyridyl))thiophene-2-carboxamide) induced a rapid-onset persistent enhancement of synaptic transmission in the dentate gyrus in vitro. Consistent with a requirement for activation of α7 nicotinic acetylcholine receptors, ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552445 Fri, 16 Dec 2011 05:00:00 +0100 5552445 http://www.medworm.com/index.php?rid=5552443&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%3D22200629%26dopt%3DAbstract Authors: Liu J, Fu S, Wei N, Hou Y, Zhang X, Cui H Abstract The bioavailabilities of eye drops are very low, so it is eager to find a safe and effective penetration enhancer to improve drug bioavailability. In our study, the corneas of New Zealand albino rabbit were mounted in the improved Franz diffusion cells for the measurement of fluconazole diffusion across the corneal permeation barrier. The fluconazole concentrations and the cumulative osmolalities were calculated to investigate the changes of permeation parameters of fluconazole through the ex vivo cornea in the presence of different penetration enhancers. Compared with the control group, 0.05% and 0.1% menthol, as well as menthol combined with borneol were considered as the penetration enhancer significantly promoted the p... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552443 Fri, 16 Dec 2011 05:00:00 +0100 5552443 http://www.medworm.com/index.php?rid=5552442&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%3D22200630%26dopt%3DAbstract Authors: Mokrushin AA, Pavlinova LI Abstract Neurotrophic and neuroprotective properties of Hsp70 were studied in olfactory cortex slices of hypertensive rats under normal conditions and under influence of autologous blood (blood clot). Under normal conditions, synaptic response in slices depended on Hsp70 amount in medium. Incubation of slices with Hsp70 showed a biphasic effect on electrogenesis in tissue. Hsp70 (from 0.1 to 3.0μg/ml) stimulated glutamatergic and GABA-ergic receptor activity. An inhibitory action on synaptic response is detected at increased amounts of Hsp70 (>4μg/ml). Pretreatment with Hsp70 (1 and 10μg/ml) prevented the irreversible inhibition of bioelectric activity in neurons damaged by autologous blood action and interfered with swelling in slices. Our... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552442 Fri, 16 Dec 2011 05:00:00 +0100 5552442 http://www.medworm.com/index.php?rid=5552451&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%3D22197001%26dopt%3DAbstract Authors: Abdin AA, Abd El-Halim MS, Hedeya SE, El-Saadany AA Abstract Rheumatoid arthritis is a chronic systemic inflammatory disease where cardiovascular diseases have been recognized as major determinants of early morbidity and mortality. Recently, there has been renewed interest in medication with glucocorticoids to decrease joint damage, but in long-term they incur substantial increase in the risk of cardiovascular diseases and their overall risk/benefit ratio is deemed unfavorable. So, the proposed role of statins in treatment of rheumatoid arthritis when corticosteroids indicated as traditional therapy needs to be investigated. Fifty albino rats were divided into 5 equal groups; normal control group, Freund's adjuvant induced arthritis group, group of induced arthritis treate... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552451 Wed, 14 Dec 2011 05:00:00 +0100 5552451 http://www.medworm.com/index.php?rid=5552450&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%3D22197002%26dopt%3DAbstract In conclusion, tramadol ameliorated cyclophosphamide-induced bladder-pain-related behaviors and bladder overactivity in rodents. These findings suggest that tramadol might be a treatment option for cystitis-induced bladder pain and bladder overactivity. PMID: 22197002 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552450 Wed, 14 Dec 2011 05:00:00 +0100 5552450 http://www.medworm.com/index.php?rid=5552448&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%3D22198047%26dopt%3DAbstract Authors: Davidson EP, Coppey LJ, Holmes A, Yorek MA Abstract Treating high fat fed/low dose streptozotocin-diabetic rats; model of type 2 diabetes, with ilepatril (vasopeptidase inhibitor, blocks neutral endopeptidase (NEP) and angiotensin converting enzyme (ACE)) improved vascular and neural functions. Next, studies were performed to determine the individual effect of inhibition of NEP and ACE on diabetes-induced vascular and neural dysfunctions. High fat fed rats (8weeks) were treated with 30mg/kg streptozotocin (i.p.) and after 4 additional weeks, were treated for 12weeks with ilepatril, enalapril (ACE inhibitor) or candoxatril (NEP inhibitor) followed by analysis of vascular and neural functions. Glucose clearance was impaired in diabetic rats and was not improved with treatmen... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5552448 Wed, 14 Dec 2011 05:00:00 +0100 5552448 http://www.medworm.com/index.php?rid=5538119&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%3D22192930%26dopt%3DAbstract Authors: Lee CH, Huang YL, Liao JF, Chiou WF Abstract We have reported previously that ugonin K, a flavonoid isolated from Helminthostachys zeylanica (L.) Hook, potently induces cell differentiation and mineralization of MC3T3-E1 mouse osteoblast-like cells. Here we aimed to elucidate whether ugonin K evoked osteogenesis required interaction with estrogen receptor. Results showed that ugonin K induced increases in alkaline phosphatase (ALP) activity, expressions of bone sialoprotein (BSP) and osteocalcin (OCN), and subsequent bone nodule formation were concentration-dependently inhibited by estrogen receptor antagonist ICI 182,780, suggesting that an estrogen receptor-dependent pathway was involved. In the presence of ICI 182,780, ugonin K induced up-regulation of the expressions o... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538119 Wed, 14 Dec 2011 05:00:00 +0100 5538119 http://www.medworm.com/index.php?rid=5538127&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%3D22173128%26dopt%3DAbstract Authors: Drube S, Schmitz F, Göpfert C, Weber F, Kamradt T Abstract The receptor tyrosine kinase c-Kit is important for mast cell differentiation, proliferation, and cytokine release. Recently, we reported that c-Kit acts as an intermediate signalling molecule regulating IL-33-induced signalling and effector functions in mast cells. Here, we investigated the influence of c-Kit on the IL-1β-induced signalling and effector functions in HMC mast cell lines. HMC-cells were stimulated with IL-1β and the resulting signalling and cytokine responses were analysed. Furthermore, we used pharmacological inhibitors to investigate the relevance of several signalling molecules for the IL-1β-induced signalling and cytokine responses. Treatment of HMC-cells with the c-Kit inhibitor STI571 bloc... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538127 Thu, 08 Dec 2011 05:00:00 +0100 5538127 http://www.medworm.com/index.php?rid=5538126&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%3D22173129%26dopt%3DAbstract Authors: Park SJ, Kim DH, Jung JM, Kim JM, Cai M, Liu X, Hong JG, Lee CH, Lee KR, Ryu JH Abstract Stigmasterol, a kind of phytosterol, is present in small amounts in various foods. In the present study, we investigated the effects of stigmasterol on scopolamine-induced memory impairments using the passive avoidance and the Morris water maze tasks in mice. In addition, changes in memory-related molecules, including extracellular signal-regulated kinase (ERK) and cAMP response element-binding protein (CREB), were examined following the administration of stigmasterol. Scopolamine-induced memory impairments were significantly attenuated by the administration of stigmasterol (10mg/kg) in the passive avoidance task. In the Morris water maze task, the escape latencies were significantly d... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538126 Thu, 08 Dec 2011 05:00:00 +0100 5538126 http://www.medworm.com/index.php?rid=5538124&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%3D22178203%26dopt%3DAbstract Authors: Harini R, Ezhumalai M, Pugalendi KV Abstract The study was designed to investigate the antihyperglycemic effect of biochanin A on streptozotocin-diabetic rats. Diabetes was induced in adult male albino rats of the Wistar strain, weighing 180-200g, by administration of streptozotocin (40mg/kg of body weight) intraperitoneally. Diabetic rats showed increase in plasma glucose and glycosylated hemoglobin and a decrease in plasma insulin and hemoglobin. Activities of gluconeogenic enzymes such as glucose 6-phosphatase, fructose 1,6-bisphosphatase increased and glucokinase, glucose 6-phosphate dehydrogenase decreased in the liver of diabetic rats along with glycogen. Oral administration of biochanin A (10mg/kg body weight) or glibenclamide (600μg/kg body weight) in 0.5% dimethy... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538124 Thu, 08 Dec 2011 05:00:00 +0100 5538124 http://www.medworm.com/index.php?rid=5538137&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%3D22166374%26dopt%3DAbstract Authors: Voss LJ, Brock M, Carlsson C, Steyn-Ross A, Steyn-Ross M, Sleigh JW Abstract Clinically, anesthetic drugs show hysteresis in the plasma drug concentrations at induction versus emergence from anesthesia induced unconsciousness. This is assumed to be the result of pharmacokinetic lag between the plasma and brain effect-site and vice versa. However, recent mathematical and experimental studies demonstrate that anesthetic hysteresis might be due in part to lag in the brain physiology, independent of drug transport delay - so-called "neural inertia". The aim of this study was to investigate neural inertia in the reduced neocortical mouse slice model. Seizure-like event (SLE) activity was generated by exposing cortical slices to no-magnesium artificial cerebrospinal fluid (aCSF)... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538137 Wed, 07 Dec 2011 05:00:00 +0100 5538137 http://www.medworm.com/index.php?rid=5538136&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%3D22166375%26dopt%3DAbstract Authors: Onishi A, Miyamae M, Kaneda K, Kotani J, Figueredo VM Abstract To assess whether sevoflurane preconditioning is associated with inhibition of mitochondrial permeability transition pore (MPTP), the effects of sevoflurane were compared with those of cyclosporine A, a known inhibitor of MPTP opening. Isolated perfused guinea pig hearts underwent 30min global ischemia and 120min reperfusion (control). Sevoflurane preconditioning was elicited by administration of 2% sevoflurane for 10min with 10min washout before ischemia (sevoflurane). A preconditioning-like cardioprotection was also induced by administering cyclosporine A (0.2μM) for 15min, starting 5min before ischemia and for 10min after the onset of reperfusion (cyclosporine A). Left ventricular developed and end-diastoli... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538136 Wed, 07 Dec 2011 05:00:00 +0100 5538136 http://www.medworm.com/index.php?rid=5538135&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%3D22166376%26dopt%3DAbstract Authors: Chen LM, Lin ZY, Zhu YG, Lin N, Zhang J, Pan XD, Chen XC Abstract The level of β-site APP-cleaving enzyme 1 (BACE1) has been documented to increase in the brains of patients with Alzheimer's disease, which has resulted in elevation of β-amyloid (Aβ) peptides. As a transcription factor binding site of the BACE1 promoter, peroxisome proliferator-activated receptor-γ (PPARγ) response element regulates the activity of the BACE1 promoter activity, indicating that PPARγ may become a potential target for Alzheimer's disease treatment. Recent studies have demonstrated that ginsenoside Rg1 which is an effective component of extracts of ginseng can prevent memory loss and improve cognitive function in a variety of animal models. However, the underlying mechanism remains unclea... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538135 Wed, 07 Dec 2011 05:00:00 +0100 5538135 http://www.medworm.com/index.php?rid=5538134&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%3D22166377%26dopt%3DAbstract In conclusion, nisoxetine had a local anesthetic effect as infiltrative cutaneous analgesia with durations of actions longer than that of lidocaine or MK-801. That N-methyl-d-aspartate receptors may not contribute to the cutaneous (local) anesthetic effect of nisoxetine or lidocaine. PMID: 22166377 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538134 Wed, 07 Dec 2011 05:00:00 +0100 5538134 http://www.medworm.com/index.php?rid=5538133&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%3D22169772%26dopt%3DAbstract In conclusion, both complexes Cu(2)(fen)(4)(dmf)(2) and Cu(2)(fen)(4)(caf)(2) were more potent antinociceptive agents than fenoprofen salt. Sub-acute exposure to different doses of these complexes did not produce significant changes in the parameters that evaluate toxicity. PMID: 22169772 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538133 Wed, 07 Dec 2011 05:00:00 +0100 5538133 http://www.medworm.com/index.php?rid=5538132&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%3D22173123%26dopt%3DAbstract In this study, we investigated the effects of intrathecal injection of a Toll-like receptor (TLR4) inhibitor epigallocatechin gallate (EGCG) on neuropathic pain induced by chronic constriction injury of the sciatic nerve (CCI). A total of 120 rats were randomly assigned into 4 groups: sham-operated group, CCI group, CCI plus normal saline group and CCI plus EGCG group. CCI and sham surgeries were performed and both thermal hyperalgesia and mechanical allodynia were tested. Lumbar spinal cord was sampled and the mRNA and protein expressions of TLR4 and High Mobility Group 1 protein (HMGB1) were detected, the contents of tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β) and interleukin-10 (IL-10) were measured by ELISA, and immunohistochemistry for nuclear factor kappa B (NF-... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538132 Wed, 07 Dec 2011 05:00:00 +0100 5538132 http://www.medworm.com/index.php?rid=5538131&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%3D22173124%26dopt%3DAbstract Authors: Kataoka T Abstract In eukaryotes, many translation inhibitors have been widely used as bioprobes to evaluate the contribution of translation to signaling pathways and cellular functions. Several types of translation inhibitors are also known to trigger the activation of the mitogen-activated protein kinase superfamily in an intracellular mechanism called ribotoxic stress response. This perspective focuses on the biological properties of recently identified translation inhibitors that trigger ribotoxic stress response, particularly glutarimides as well as triene-ansamycins. PMID: 22173124 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538131 Wed, 07 Dec 2011 05:00:00 +0100 5538131 http://www.medworm.com/index.php?rid=5538129&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%3D22173126%26dopt%3DAbstract Authors: Assaly R, de Tassigny AD, Paradis S, Jacquin S, Berdeaux A, Morin D Abstract Reactive oxygen species production is necessary to induce cell death following hypoxia/reoxygenation but the effect of reactive oxygen species produced during hypoxia on mitochondrial permeability transition pore (mPTP) opening and cell death is not established. Here we designed a model of hypoxia/reoxygenation in isolated cardiomyocytes measuring simultaneously reactive oxygen species production, mPTP opening and cell death in order (i) to establish a causal relationship between them, and (ii) to investigate the roles of various reactive oxygen species in mPTP opening. The percentage of cardiomyocytes exhibiting mPTP opening during reoxygenation increased with the duration of hypoxia. Antioxidant... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538129 Wed, 07 Dec 2011 05:00:00 +0100 5538129 http://www.medworm.com/index.php?rid=5538128&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%3D22173127%26dopt%3DAbstract Authors: Na HS, Park HP, Kim CS, Do SH, Zuo Z, Kim CS Abstract Estrogen, a neuroactive sex hormone in the brain, enhances neuronal excitability and increases seizures. Glutamate transporters help in limiting the excitatory neurotransmission by uptaking glutamate from the synapses. We investigated the effects of 17β-estradiol on the activity of a glutamate transporter, excitatory amino acid transporter 3 (EAAT3), in Xenopus oocytes. EAAT3 was expressed in Xenopus oocytes by injection of rat EAAT3 mRNA. l-Glutamate (30μM)-induced membrane currents mediated by EAAT3 were measured using the two-electrode voltage clamp technique. 17β-Estradiol reduced EAAT3 activity in a concentration- and time-dependent manner. 17β-Estradiol (10nM for 72h) significantly decreased V(max) but had no ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538128 Wed, 07 Dec 2011 05:00:00 +0100 5538128 http://www.medworm.com/index.php?rid=5538125&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%3D22173130%26dopt%3DAbstract Authors: Madeira JM, Beloukhina N, Boudreau K, Boettcher TA, Gurley L, Walker DG, McNeil WS, Klegeris A Abstract Neuroinflammation contributes to the pathogenesis of neurological disorders including stroke, head trauma, multiple sclerosis, amyotrophic lateral sclerosis as well as age-associated neurodegenerative disorders including Alzheimer's and Parkinson's diseases. Therefore, anti-inflammatory drugs could be used to slow the progression of these diseases. We studied the anti-neuroinflammatory activity of four novel square planar cobalt(II) compounds bearing tetradentate β-ketoaminato ligands with variation in the number of CF(3) ligand substituents, as well as their corresponding unmetallated organic ligands. Cobalt (Co) complexes were consistently more active than their corre... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538125 Wed, 07 Dec 2011 05:00:00 +0100 5538125 http://www.medworm.com/index.php?rid=5538122&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%3D22178922%26dopt%3DAbstract Authors: Wiegand V, Gimpl G Abstract The oxytocin receptor specifically requires cholesterol to maintain and stabilize its high-affinity agonist binding. Here, we applied a receptor chimeric approach to coarsely localize the cholesterol binding domain of the oxytocin receptor. During these studies, we identified the specific dependence on cholesterol as a common property of the oxytocin-vasopressin receptor family. We asked whether the oxytocin receptor maintains or loses its cholesterol dependence when parts of the receptor are exchanged by the corresponding fragments of the cholecystokinin receptor that does not show a specific cholesterol dependence. One of the chimeric receptors revealed full oxytocin binding activity, was capable of signal transduction, and its cholesterol dep... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538122 Wed, 07 Dec 2011 05:00:00 +0100 5538122 http://www.medworm.com/index.php?rid=5538121&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%3D22178923%26dopt%3DAbstract This study may have a significant impact on myocardial infarction. PMID: 22178923 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538121 Wed, 07 Dec 2011 05:00:00 +0100 5538121 http://www.medworm.com/index.php?rid=5538120&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%3D22182582%26dopt%3DAbstract In this study, we therefore investigated the structure-specific for eliciting the neuroprotective effect by examining a series of NSAIDs against MPP(+) toxicity in SH-SY5Y cells. Three oxicam-bearing NSAIDs showed potent neuroprotective effects, although none of the other 10 oxicam-nonbearing NSAIDs (3 salicylates, 6 coxibs and 1 polyphenol) or 3 piroxicam analogs (including ampiroxicam, a precursor of piroxicam) exerted any neuroprotection. Tenoxicam and piroxicam prevented MPP(+)-induced reduction of phosphorylated Akt levels in cells: a protective mechanism similar to that of meloxicam. Therefore, the oxicam structure was likely to be responsible for exhibiting the neuroprotection by sustaining survival-signaling in dopaminergic cells. The present results raise the possibility that the ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538120 Wed, 07 Dec 2011 05:00:00 +0100 5538120 http://www.medworm.com/index.php?rid=5538130&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%3D22173125%26dopt%3DAbstract Authors: Stieger B, Heger M, de Graaf W, Paumgartner G, van Gulik T Abstract Liver function tests are of critical importance for the management of patients with severe or terminal liver disease. They are also used as prognostic tools for planning liver resections. In recent years many transport systems have been identified that also transport substances employed in liver function tests. Such substances include endogenous bilirubin or exogenously administered indocyanine green, agents for magnetic resonance imaging, agents for single photon emission computed tomography or agents for breath tests. The increasing functional and molecular information on the respective transport systems should improve the management and as a result the outcome of patients scheduled for liver surgery or ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538130 Tue, 06 Dec 2011 05:00:00 +0100 5538130 http://www.medworm.com/index.php?rid=5538138&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%3D22155399%26dopt%3DAbstract In conclusion, [(3)H]Lu AE60157 is suitable for measuring in vivo occupancies of 5-HT(6) receptor ligands in rat brain regions in which 5-HT(2A) receptors do not interfere. PMID: 22155399 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538138 Sun, 04 Dec 2011 05:00:00 +0100 5538138 http://www.medworm.com/index.php?rid=5538123&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%3D22178921%26dopt%3DAbstract In conclusion, intra-VL PAG PEA induces antinociceptive effects associated with a decrease in RVM ON and OFF cell activities. PPAR-α receptors mediate, and CB(1) and TRPV(1) receptors antagonise, PEA-induced effects within the PAG-RVM circuitry. PMID: 22178921 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538123 Sat, 03 Dec 2011 05:00:00 +0100 5538123 http://www.medworm.com/index.php?rid=5538140&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%3D22154756%26dopt%3DAbstract Authors: Wheal AJ, Alexander SP, Randall MD Abstract Hydrogen peroxide (H(2)O(2)) has been shown to participate in endothelium-derived hyperpolarising factor (EDHF)-mediated mechanisms. Vasorelaxation to the endocannabinoid-like N-oleoylethanolamine (OEA) and anandamide has been shown to be endothelium-dependent. Therefore, the principal aim was to investigate whether H(2)O(2) plays a role in vasorelaxation to endocannabinoids in rat mesenteric arteries. We have also investigated the effects of catalase on endothelium-dependent relaxations and vascular responses to H(2)O(2). First- (G1) and third- (G3) order branches of the superior mesenteric artery from male, Wistar rats were mounted in a wire myograph, contracted with methoxamine, and concentration-response curves to anandamide,... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538140 Tue, 29 Nov 2011 05:00:00 +0100 5538140 http://www.medworm.com/index.php?rid=5538139&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%3D22154757%26dopt%3DAbstract Authors: Kumar P, Kalonia H, Kumar A Abstract Huntington's disease is a progressive neurodegenerative disorder that gradually reduces memory, cognitive skills and normal movements of affected individuals. Systemic administration of 3-Nitropropionic acid induces selective striatal lesions in rodents and non-human primates. Therefore, the present study has been designed to elucidate the comparative mechanistic profile of gabapentin, lamotrigine and their interactions with GABAergic modulators against 3-Nitropropionic acid induced neurotoxicity. Systemic 3-Nitropropionic acid (10mg/kg) administration for 14days significantly reduced body weight, locomotor activity, grip strength, oxidative defense (LPO, nitrite, SOD and catalase) and impaired mitochondrial complex enzyme (I, II, IV an... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5538139 Mon, 28 Nov 2011 05:00:00 +0100 5538139 http://www.medworm.com/index.php?rid=5478602&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%3D22142993%26dopt%3DAbstract Authors: Houston AJ, Wong JC, Ebenezer IS Abstract The effects of subcutaneous (s.c.) administration of the GABA(B) receptor agonist baclofen were investigated on primary drinking in rats. Baclofen (1-4mg/kg) produced a dose-related reduction in cumulative water intake in 16h water-deprived rats during the 120min measurement period (Experiment 1). The suppressant effect of baclofen (2mg/kg) on water intake 16h water-deprived rats was significantly attenuated by pretreatment with the GABA(B) receptor antagonist CGP 35348 (3-aminopropyl (diethoxymethyl)-phosphinic acid; 50mg/kg; s.c., Experiment 2.), indicating that the hypodipsic effects of the drug in thirsty rats are mediated by an action at GABA(B) receptors. Experiment 3 was undertaken to investigate the effects of baclofen on v... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478602 Mon, 28 Nov 2011 05:00:00 +0100 5478602 http://www.medworm.com/index.php?rid=5478604&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%3D22134006%26dopt%3DAbstract Authors: Pacheco DD, Pacheco CM, Duarte ID Abstract Studies have demonstrated that the L-arginine/NO/cGMP pathway and the potassium and calcium channels are involved in the mechanisms underlying opioid receptor activation. As additional pathways may participate in the observed antinociceptive effects following opioid exposure, the aim of our study was to determine whether Ca(2+)-activated Cl(-) channels (CaCCs) are involved in peripheral antinociception induced by μ-, δ- and κ-opioid receptor activation. Hyperalgesia was induced by intraplantar injection of prostaglandin E(2) (PGE(2), 2μg). Nociceptive thresholds to pressure (grams) were measured using an algesimetric apparatus 3h following injection. The μ-opioid receptor agonist morphine (200μg), δ-opioid receptor agonist ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478604 Sun, 27 Nov 2011 05:00:00 +0100 5478604 http://www.medworm.com/index.php?rid=5478603&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%3D22142992%26dopt%3DAbstract Authors: Anand R, Gulati K, Ray A Abstract The present study evaluated the effects of the opioid agonist, morphine on stress induced anxiogenesis and the possible involvement of nitric oxide (NO) in such effects in rats. Acute restraint stress consistently induced an anxiety-like response in the elevated plus maze test, i.e. reduced number of open arm entries and time spent in the open arms as compared to controls. Pretreatment with morphine (1 and 5mg/kg), attenuated the restraint stress induced anxiogenic response in a dose related manner. Restraint stress induced neurobehavioral suppression was associated with reductions in brain NO oxidation products (NOx) levels, which were also reversed with morphine. Interaction studies showed that sub-effective doses of morphine and l-argin... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478603 Sun, 27 Nov 2011 05:00:00 +0100 5478603 http://www.medworm.com/index.php?rid=5478610&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%3D22127324%26dopt%3DAbstract Authors: Zhou J, Zhou S, Gao Y, Zeng S Abstract Quercetin is an active constituent of Hippophae rhamnoides L. and Ginkgo Biloba, which are commonly taken for high altitude sickness. The preventive effect of quercetin on hypobaric hypoxic rats was investigated. Male Wistar rats (180-220g) were placed into six groups: normoxic group (normal control), a hypoxic group (model control), three quercetin-treated groups (5, 10, 20mg/kg, i.g.), and acetazolamide-treated group (22.5mg/kg, i.g., positive control), 10 animals in each group. Hypoxic rats were raised in a hypobaric hypoxia chamber simulating a high altitude of 5000m for 23h per day after a five-day pretreatment. Normoxic control rats were raised at an altitude of 300m. After the five-day treatment, hemodynamic, arterial blood gas... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478610 Fri, 25 Nov 2011 05:00:00 +0100 5478610 http://www.medworm.com/index.php?rid=5478621&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%3D22119078%26dopt%3DAbstract In this study, kindling was induced by administration of subconvulsive dose of pentylenetetrazol (35mg/kg; i.p.) on alternate days in mice of different age group (2, 6 and 12month old). For the evaluation of short term, long term spatial and contextual fear memory Elevated Plus Maze and Passive Shock Avoidance Paradigm were used respectively. Induction of kindling significantly impaired learning and memory in different age group of mice as compared to their naïve. Kindling also affected the working and reference spatial memory, with function of age in kindled mice, and contextual fear memory in kindled mice, however not in age dependent manner. Thus the present study validated the existence of age dependent differences in learning and memory deficit and induction of kindling in mice. Resu... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478621 Wed, 23 Nov 2011 05:00:00 +0100 5478621 http://www.medworm.com/index.php?rid=5478609&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%3D22130356%26dopt%3DAbstract In conclusion, protection against osteoporosis by statins is linked to a reduction of oxidative stress and restoration of NO formation in aged and ovariectomized rats. PMID: 22130356 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478609 Wed, 23 Nov 2011 05:00:00 +0100 5478609 http://www.medworm.com/index.php?rid=5478608&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%3D22130357%26dopt%3DAbstract Authors: Baek YY, Cho DH, Choe J, Lee H, Jeoung D, Ha KS, Won MH, Kwon YG, Kim YM Abstract Taurine, a non essential sulfur-containing amino acid, plays a critical role in cardiovascular functions. We here examined the effect of taurine on angiogenesis and its underlying signal pathway. Taurine treatment increased angiogenesis in vitro and in vivo, which was followed by activation of the phosphatidylinositol 3-kinase (PI3K)/Akt, MEK/ERK, and Src/FAK signaling pathways. Further, taurine promoted endothelial cell cycle progression to the S and G2/M phases by up-regulating the positive cell cycle proteins, particularly cyclins D1 and B, as well as down-regulating the negative cell cycle proteins, p53 and p21(WAF1/CIP1), resulting in Rb phosphorylation. This angiogenic event was inhibit... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478608 Wed, 23 Nov 2011 05:00:00 +0100 5478608 http://www.medworm.com/index.php?rid=5478607&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%3D22134003%26dopt%3DAbstract Authors: Hamidi GA, Ramezani MH, Arani MN, Talaie SA, Banafshe HR Abstract Neuropathic pain is caused by a lesion or disease of the somatosensory nervous system and treatment of neuropathic pain remains a challenge. The purpose of the present study was to examine the effect of ethosuximide, an anti-epileptic and relatively selective T-type calcium blocker and morphine, a prototypical opioid in the behavioral responses following the chronic constriction injury (CCI) model of neuropathic pain. Experiments were performed on eight groups (n=8) of male Sprague-Dawley rats (230-280g). The animals were injected with saline, ethosuximide (100, 200, 300mg/kg), morphine (4mg/kg), and a combination of morphine (4mg/kg) plus ethosuximide (100mg/kg, i.p.). The cold-and mechano-allodynia and the... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478607 Wed, 23 Nov 2011 05:00:00 +0100 5478607 http://www.medworm.com/index.php?rid=5478605&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%3D22134005%26dopt%3DAbstract Authors: Narayana K, Al-Bader M, Mousa A, Khan KM Abstract Cisplatin-based chemotherapy regimens are preferred in the treatment of a variety of cancers. The present study investigated early cumulative molecular effects of therapeutic dose-levels of bleomycin, etoposide and cisplatin (BEP) in the testis and their modulation by an antioxidant cocktail (AO). Adult male Sprague-Dawley rats (N=7/group [G]) were treated with BEP as follows: G1 - control; G2 - AO (α-tocopherol [100mg/kg], l-ascorbic acid [50mg/kg], Zn [40mg/l] and Se [100μg/l]); G3 - B, 1.5mg/kg on day 2; E, 15mg/kg and P, 3mg/kg for 4days, and G4 - similar to G3 but also treated with AO for 4days. In G3, the testis weight, sperm count and motility, and activities of enzymatic antioxidants decreased and lipid peroxidati... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478605 Wed, 23 Nov 2011 05:00:00 +0100 5478605 http://www.medworm.com/index.php?rid=5478617&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%3D22119379%26dopt%3DAbstract Authors: Taniguchi M, Arai N, Kohno K, Ushio S, Fukuda S Abstract A stable ascorbic acid derivative, 2-O-α-glucopyranosyl-l-ascorbic acid (AA-2G), was evaluated and compared with ascorbic acid for its protective effect against cellular damage and senescence induced by hydrogen peroxide (H(2)O(2)). Pretreatment with AA-2G for 72h promoted the proliferation of normal human dermal fibroblasts (NHDF) and protected against cell damage induced by H(2)O(2). In contrast, ascorbic acid increased the proliferation and protected against cell damage, only when culture medium containing ascorbic acid was replaced every 24h during the pretreatment period. These results suggest that the effect of AA-2G is longer-lasting compared to that of ascorbic acid. Senescence associated-β-galactosidase (S... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478617 Mon, 21 Nov 2011 05:00:00 +0100 5478617 http://www.medworm.com/index.php?rid=5478606&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%3D22134004%26dopt%3DAbstract Authors: Alcántara Hernández R, García-Sáinz JA Abstract The role of phosphoinositide-dependent protein kinase-1 (PDK-1) activity on α(1B)-adrenoceptor phosphorylation and function was explored using pharmacological inhibitors and expression of a dominant-negative mutant of this enzyme. Noradrenaline-, phorbol myristate acetate-, lysophosphatidic acid- and epidermal growth factor-mediated α(1B)-adrenoceptor phosphorylation were markedly reduced by the two inhibitors used: UCN-01 [(7-hydroxystaurosporine; (3R*,8S*, 9R*, 10R*,12R*)-2,3,9,10,11,12-hexahydro-3-hydroxy-9-methoxy-8-methyl-10-(methylamino)-8,12-epoxy-1H, 8H-2,7b,12a-triazadibenzo[a,g]-cyclonona[cde]triden-1-one)] and OSU-03012 [(2-amino-N-[4-[5-(2-phenanthrenyl)-3-trifluoromethyl)-1H-pyrazol-1-yl]pnehyl]-acetamide)]... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478606 Mon, 21 Nov 2011 05:00:00 +0100 5478606 http://www.medworm.com/index.php?rid=5478620&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%3D22119079%26dopt%3DAbstract Authors: Hu J, Chai Y, Wang Y, Kheir MM, Li H, Yuan Z, Wan H, Xing D, Lei F, Du L Abstract Berberine is a candidate clinical neuroprotective agent against ischemic stroke. In the present study, we examined the influence of the PI3K/Akt pathway in mediating the anti-apoptotic effects of berberine. Oxygen-glucose deprivation and reoxygenation of nerve growth factor-differentiated PC12 cells and primary neurons, and bilateral common carotid artery occlusion in mice were used as in vitro and in vivo ischemia models. We found that the anti-apoptotic effects of berberine against ischemia were indeed mediated by the increased phosphor-activation of Akt (higher p-Akt to total Akt), leading to the intensified phosphorylation of Bad and the decreased cleavage of the pro-apoptotic protease ca... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478620 Sat, 19 Nov 2011 05:00:00 +0100 5478620 http://www.medworm.com/index.php?rid=5478619&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%3D22119377%26dopt%3DAbstract In this study, this lichen metabolite and olive oil activated caspase-dependent cell death with apoptotic morphology, which is distinctly different from necrosis. Both orally and locally administered olive oil and diffractaic acid exerted pro-apoptotic induction in tissues surrounding the implants in titanium-implanted rabbits through the activation of initiator caspases (Cas-2, -8 and -9) and executioner caspase (Cas-3). In addition, they displayed strong myeloperoxidase and inducible nitric oxide synthase activities, providing an alleviating effect. Furthermore, administrations of diffractaic acid and olive oil attenuated the Ti-alloy implantation, and decreased superoxide dismutase activity and total glutathione level in peri-implant tissues. These results demonstrate that diffractaic a... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478619 Sat, 19 Nov 2011 05:00:00 +0100 5478619 http://www.medworm.com/index.php?rid=5478618&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%3D22119378%26dopt%3DAbstract Authors: Moro C, Leeds C, Chess-Williams R Abstract In the bladder, nitric oxide (NO) is released from neuronal and non-neuronal sources, but its actions are unclear. Strips of urothelium plus lamina propria contract in response to agonists and develop spontaneous phasic contractions, and the aim of this study was to investigate the influence of NO on this activity. Isolated strips of urothelium/lamina propria from porcine bladder developed spontaneous contractions (3.5±0.3cycles/min) and contracted in response to carbachol and electrical field stimulation (EFS). The NO synthase inhibitor N(ω)-nitro-l-arginine (L-NNA, 100μM) had no effects on the tissues, but the NO donors diethylamine NONOate (DEANO, 100μM) and nitroprusside (10μM) caused relaxation, slowed the spontaneous ra... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478618 Sat, 19 Nov 2011 05:00:00 +0100 5478618 http://www.medworm.com/index.php?rid=5478616&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%3D22119380%26dopt%3DAbstract Authors: Flores-Soto E, Reyes-García J, Sommer B, Chavez J, Barajas-López C, Montaño LM Abstract The Na(+)/Ca(2+)exchanger (NCX) principal function is taking 1 Ca(2+) out of the cytoplasm and introducing 3 Na(+). The increase of cytoplasmic Na(+) concentration induces the NCX reverse mode (NCX(REV)), favoring Ca(2+) influx. NCX(REV) can be inhibited by: KB-R7943 a non-specific compound that blocks voltage-dependent and store-operated Ca(2+) channels; SEA0400 that appears to be selective for NCX(REV), but difficult to obtain and SN-6, which efficacy has been shown only in cardiomyocytes. We found that PPADS, a P2X receptor antagonist, acts as a NCX(REV) inhibitor in guinea pig tracheal myocytes. In these cells, we characterized the NCX(REV) by substituting NaCl and NaHCO(3) with ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478616 Sat, 19 Nov 2011 05:00:00 +0100 5478616 http://www.medworm.com/index.php?rid=5478615&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%3D22119381%26dopt%3DAbstract In this report, we evaluated the effect of APO866, a potent inhibitor of NAMPT against C6 glioblastoma. We found that APO866 inhibited the growth of C6 glioblastoma cells with IC(50) in nano-molar range. APO866 depleted intracellular NAD, caused marked inhibition of ERK activation and induced G2/M cell-cycle arrest. The effects by APO866 were abrogated by nicotinamide mononucleotide (NMN), the direct product of NAMPT. Administration of U0126, an ERK1/2 inhibitor, inhibited cell growth but displayed no synergistic effect with APO866. Taken together, our results indicated that APO866 is a potent growth inhibitor against glioblastoma through targeting NAMPT. PMID: 22119381 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478615 Sat, 19 Nov 2011 05:00:00 +0100 5478615 http://www.medworm.com/index.php?rid=5478613&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%3D22119383%26dopt%3DAbstract Authors: Graziosi L, Mencarelli A, Santorelli C, Renga B, Cipriani S, Cavazzoni E, Palladino G, Laufer S, Burnet M, Donini A, Fiorucci S Abstract Peritoneal dissemination is a highly frequent complication of poorly differentiated gastric cancers for which no effective therapies are available. Constitutive activation of mitogen-activated protein kinases (MAPKs) signaling cascades is recognized as a causative factor in the malignant transformation of several carcinoma cell types. In the present study we provide evidence that p38 MAPK inhibition protects against gastric cancer cells dissemination in a mouse model of peritoneal carcinomatosis. Administering mice with ML3403 and SB203580, potent and selective p38 MAPK inhibitors, attenuate the formation of neoplastic foci induced by int... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478613 Sat, 19 Nov 2011 05:00:00 +0100 5478613 http://www.medworm.com/index.php?rid=5478614&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%3D22119382%26dopt%3DAbstract Authors: Wu Y, Li Y, Gao J, Sui N Abstract Dysfunctional reconsolidation processes may help drug memories resist extinction and contribute to high rate of relapse. Reconsolidation of drug memory is mainly affected by the appetitive and aversive emotional experiences associated with an addictive drug. The nucleus accumbens has been shown to mediate the reconsolidation of positive emotional addictive memory, but its role in negative emotional addictive memory remains elusive. In the present study, we used morphine-induced CPP (m-CPP) and morphine-naloxone induced conditioned place aversion (m-CPA) to investigate the role of N-methyl-d-aspartate (NMDA) receptors within the nucleus accumbens on reconsolidation of emotional drug memory. Here we demonstrate that infusion of the NMDA rece... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478614 Fri, 18 Nov 2011 05:00:00 +0100 5478614 http://www.medworm.com/index.php?rid=5478612&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%3D22119384%26dopt%3DAbstract Authors: Karlsson LO, Bergh N, Li L, Bissessar E, Bobrova I, Gross GJ, Akyürek LM, Grip L Abstract Opioids confer cardioprotection after myocardial ischaemia and reperfusion. The primary aim of the present study was to evaluate the cardioprotective effect of different doses of enkephalin analogue Eribis peptide 94 (EP 94) in a porcine model of ischaemia and reperfusion. A secondary aim was to analyse the impact of ischaemia and reperfusion on the expression of opioid receptor subtypes in the porcine heart. Thirty-four anesthetised pigs underwent 40min of balloon occlusion of the left anterior descending coronary artery followed by four hours of reperfusion. Pigs were given either vehicle (0.9% NaCl) or one of four doses of EP 94 (0.2, 1, 5 or 25ug/kg at each administration, respec... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478612 Wed, 16 Nov 2011 05:00:00 +0100 5478612 http://www.medworm.com/index.php?rid=5478611&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%3D22119385%26dopt%3DAbstract This study indicates that DMF effectively modulates the regulation of anti-oxidative and anti-inflammatory action, via up-regulation of HO-1 in HT22 cells and BV2 microglia. These results suggest that DMF possesses therapeutic potentials against neurodegenerative diseases that are induced by oxidative stress and neuroinflammation. PMID: 22119385 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478611 Wed, 16 Nov 2011 05:00:00 +0100 5478611 http://www.medworm.com/index.php?rid=5478627&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%3D22115891%26dopt%3DAbstract Authors: Kostrzewa-Nowak D, Bieg B, Paine MJ, Wolf CR, Tarasiuk J Abstract Clinical usefulness of anthracyclines belonging to bioreductive antitumour drugs is limited by the occurrence of multidrug resistance (MDR). The aim of this study was to examine the role of structural factors of antitumour anthracycline drugs in the ability to undergo bioreductive activation by NADPH cytochrome P450 reductase (CPR) and determine the impact of this activation on increasing the activity especially in regard to MDR tumour cells. It was evidenced that at high NADPH concentration (500μM) anthracyclines having non-modified quinone structure: doxorubicin (DOX), daunorubicin (DR) and idarubicin (IDA) were susceptible upon CPR catalysis to undergo a multi-stage chemical transformation concerning the... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478627 Tue, 15 Nov 2011 05:00:00 +0100 5478627 http://www.medworm.com/index.php?rid=5478630&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%3D22101231%26dopt%3DAbstract Authors: Acewicz A, Mierzejewski P, Dyr W, Jastrzebska A, Korkosz I, Wyszogrodzka E, Nauman P, Samochowiec J, Kostowski W, Bienkowski P Abstract Individuals prone to drug self-administration may be vulnerable not only to a single drug reinforcer but to a variety of drug reinforcers. It has been shown that two thirds of alcoholics regularly use drugs other than ethanol (alcohol). Up to 30% of alcohol-dependent patients report concurrent misuse of cocaine. The aim of the present study was to investigate intravenous cocaine self-administration in selectively bred, alcohol-preferring WHP (Warsaw high-preferring) and non-preferring WLP (Warsaw low-preferring) rats. It was hypothesized that WHPs could be more prone to cocaine self-administration in comparison to WLPs. Rats from both line... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478630 Sat, 12 Nov 2011 05:00:00 +0100 5478630 http://www.medworm.com/index.php?rid=5478629&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%3D22108548%26dopt%3DAbstract Authors: Vuaden FC, Savio LE, Ramos DB, Casali EA, Bogo MR, Bonan CD Abstract Extracellular adenosine 5'-triphosphate (ATP) acts as a proinflammatory mediator. Adenosine, the final product of ATP breakdown, is an anti-inflammatory compound, acting mainly on adenosine A(2A) receptors. Considering that the kidney is an organ strongly affected during systemic inflammatory responses and that ectonucleotidases are responsible for the control of extracellular nucleotide and nucleoside levels, we examined the endotoxin-induced effects on ectonucleotidases in kidney membranes of mice, and whether CGS-21680 hydrochloride (3-[4-[2-[[6-amino-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxy-oxolan-2-yl]purin-2-yl]amino]ethyl]phenyl]propanoic acid), a selective adenosine A(2A) receptor agonist... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478629 Sat, 12 Nov 2011 05:00:00 +0100 5478629 http://www.medworm.com/index.php?rid=5478628&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%3D22108549%26dopt%3DAbstract Authors: Decaluwé K, Pauwels B, Verpoest S, Van de Voorde J Abstract Carbon monoxide (CO) may play an important physiological role in regulation of the vascular tone. CO-releasing molecule (CORM-2) is frequently used as a CO-donor to evaluate (patho)physiological properties of CO and its potential therapeutic applications. The aim of this study was to examine the molecular mechanisms underlying the vasodilatory properties of CORM-2 as this has not yet been extensively explored. Isometric tension recordings were performed using mice and rat isolated aortic ring segments as well as mice femoral artery ring segments. Responses to CO (10μmol/l-300μmol/l) and CORM-2 (30μmol/l-600μmol/l) were evaluated in the presence/absence of activators/inhibitors of different molecular pathways.... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478628 Sat, 12 Nov 2011 05:00:00 +0100 5478628 http://www.medworm.com/index.php?rid=5478626&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%3D22115892%26dopt%3DAbstract Authors: Gonçalves AE, Bürger C, Amoah SK, Tolardo R, Biavatti MW, de Souza MM Abstract We have recently shown that the ethanol extract of the leaves of Hedyosmum brasiliense exhibits an antidepressant-like effect in the tail suspension and forced swimming tests in mice. The present study investigates the mechanisms involved in the antidepressant-like effect of H. brasiliense extract, together with the antidepressant potential of podoandin, an isolated sesquiterpenoid. H. brasiliense (50mg/kg, i.p.) and podoandin (10mg/kg, i.p.) decreased the immobility time in the forced swimming test, without any accompanying changes in ambulation in the open-field test. The anti-immobility effect of the H. brasiliense extract was prevented by pre-treating the mice with ondansetron, NAN 190, pi... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478626 Sat, 12 Nov 2011 05:00:00 +0100 5478626 http://www.medworm.com/index.php?rid=5478625&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%3D22115893%26dopt%3DAbstract Authors: Sangeetha N, Viswanathan P, Balasubramanian T, Nalini N Abstract Our findings reported so far demonstrate that silibinin modulates gut microbial enzymes, colonic oxidative stress and Wnt/β-catenin signaling, to exert its antiproliferative effect against 1,2 di-methylhydrazine (DMH) induced colon carcinogenesis. Since xenobiotic metabolizing enzymes play a crucial role in carcinogen activation and metabolism, we aimed to explore the effect of silibinin on xenobiotic metabolizing enzymes during DMH induced colon carcinogenesis. Male albino rats were randomly divided into six groups. Group 1 served as control and group 2 rats received 50mg/kg body weight of silibinin p.o. every day. Groups 3-6 rats were given DMH at a dose of (20mg/kg body weight subcutaneously) once a week ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478625 Sat, 12 Nov 2011 05:00:00 +0100 5478625 http://www.medworm.com/index.php?rid=5478624&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%3D22115894%26dopt%3DAbstract Authors: Maggo S, Clark D, Ashton JC Abstract Statins play a crucial role in reducing the risk of death from cardiovascular disease in millions of people worldwide. Recently, pharmacovigilance data has suggested that statin drugs may have rare but significant adverse psychiatric effects, such as amnesia, anxiety and even aggression. In order to investigate the effects of statins on cognitive function in an animal model, we studied the effect of 6weeks of daily administration of oral simvastatin (1mg/kg) or atorvastatin (0.5mg/kg) in guinea pig on performance in the Morris water maze (MWM). Animals were also re-tested in the MWM, 2weeks after drug cessation, to test for any changes in performance as a result of drug de-challenge. Guinea pigs treated with either statin showed a signi... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478624 Sat, 12 Nov 2011 05:00:00 +0100 5478624 http://www.medworm.com/index.php?rid=5478623&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%3D22115895%26dopt%3DAbstract Authors: Li L, Zhang ZF, Holscher C, Gao C, Jiang YH, Liu YZ Abstract It has being shown that glucagon-like peptide-1 (GLP-1), a new anti-diabetes agent, significantly attenuated beta-amyloid (Aβ) levels in rats. In the present study, (Val(8))GLP-1 was used to prevent impairments in memory formation, tau hyperphosphorylation and ultra-structural changes induced by streptozotocin intracerebroventricular (i.c.v.) injection. A spatial water maze task was used to test the rats' learning and memory formation, Western blot was used to measure tau hyperphosphorylation/total tau, and transmission electron microscope was used to find ultra-structural changes. The results shown that streptozotocin induced a series of Alzheimer disease -like changes in behaviour, a significant decline in lea... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478623 Sat, 12 Nov 2011 05:00:00 +0100 5478623 http://www.medworm.com/index.php?rid=5478622&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%3D22115896%26dopt%3DAbstract Authors: Faivre E, Hamilton A, Hölscher C Abstract Type 2 diabetes is a risk factor for Alzheimer's disease. Insulin receptor desensitisation has been found in Alzheimer brains, which may be the underlying link. Glucose-dependent insulinotropic polypeptide (GIP), an incretin hormone, normalises insulin signalling in diabetes. GIP and the GIP receptors are widely expressed in the brain, and GIP has been shown to have growth factor and neuroprotective properties. Here we investigate the potential therapeutic properties of different doses of the protease resistant long-lasting GIP receptor agonist D-Ala2GIP and the antagonist (Pro3)GIP in C57Bl/6 mice. We found that after acute injection, D-Ala2GIP had few effects on general behaviour in the open field at any dose tested (2.5, 25, 10... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5478622 Sat, 12 Nov 2011 05:00:00 +0100 5478622 http://www.medworm.com/index.php?rid=5427225&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%3D22088276%26dopt%3DAbstract Authors: Chen W, Tang F, Xie B, Chen S, Huang H, Liu P Abstract Oxidative stress plays a crucial role in atherogenesis, which raises the possibility of using antioxidants to ameliorate atherosclerosis. In the present study, we aim to determine the effects of tanshinone IIA (TSIIA) on atherosclerosis in hyperlipidemic rabbits. After feeding the rabbits on a high-lipid diet for 90days, they developed severe atherosclerotic lesions both morphologically and biochemically and exhibited significantly elevated serum lipid, malondialdehyde (MDA) and oxidized low density lipoprotein (oxLDL) levels. Oral administration of TSIIA (3-30mg/kg) greatly inhibited the formation of atherosclerotic lesions. In TSIIA-treated rabbits, there was a marked reduction in serum and aortic lipid peroxide prod... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427225 Wed, 09 Nov 2011 05:00:00 +0100 5427225 http://www.medworm.com/index.php?rid=5427224&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%3D22094060%26dopt%3DAbstract In this study, we first confirmed the statin-induced autophagy by assessing other criteria, including induced expression of the autophagy-related genes, enhanced protein degradation of autophagy marker protein p62 and electron microscopic observation of induced formation of autophagosome. We next demonstrated that the extent of inhibition of HMG-CoA reductase in the cell is parallel with the ability of a statin to induce autophagy. Thus, the primary activity of statins causes autophagy in A204 cells. Considering the mechanism for the induction, we showed that statins induce autophagy by depleting cellular levels of geranylgeranyl diphosphate (GGPP) mostly through an unknown pathway that does not involve two major small G proteins, Rheb and Ras. Finally, we demonstrated that the ability of ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427224 Wed, 09 Nov 2011 05:00:00 +0100 5427224 http://www.medworm.com/index.php?rid=5427223&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%3D22094061%26dopt%3DAbstract Authors: Lelliott A, Nikkar-Esfahani A, Offer J, Orchard P, Roberts RE Abstract Extracellular signal regulated kinase (ERK) is known to regulate vascular smooth muscle contraction. However, a role for ERK in airway smooth muscle contraction has yet to be demonstrated conclusively, although contractile agents increase ERK activity in airway smooth muscle. Rather than initiating contraction, ERK could regulate airway tone by interfering with relaxation. Therefore, the aim of this study was to determine whether ERK regulates contraction or relaxation of airway smooth muscle. Segments of porcine peripheral bronchioles were mounted in an isolated tissue bath in Krebs-Henseleit buffer and maintained at 37°C. Cumulative concentration-response curves to histamine, endothelin-1, or the mus... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427223 Wed, 09 Nov 2011 05:00:00 +0100 5427223 http://www.medworm.com/index.php?rid=5427222&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%3D22094062%26dopt%3DAbstract Authors: Ahmad A, Mondello S, Di Paola R, Mazzon E, Esposito E, Catania MA, Italiano D, Mondello P, Aloisi C, Cuzzocrea S Abstract The aim of this study was to investigate the effects of apocynin, a NADPH (nicotinamide adenine dinucleotide phosphate)-oxidase inhibitor, in diabetic rats with nephropathy induced by contrast medium (CIN). Diabetes was induced in male Wistar rats by a single dose of streptozotocin (60mg/kg i.v.). Animals were then divided into the following groups: 1) control group (diabetic rats treated i.v. with saline solution); 2) iomeprol group (iomeprol at 10ml/kg was injected i.v. 30min after saline administration); 3) apocynin group (identical to the iomeprol group, except for pre-treatment with apocynin 5mg/kg i.v., 30min before iomeprol injection) and 4) N-ac... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427222 Wed, 09 Nov 2011 05:00:00 +0100 5427222 http://www.medworm.com/index.php?rid=5427221&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%3D22094063%26dopt%3DAbstract In conclusion, PDE5 inhibitors applied luminally had minor contractile effect, whereas abluminal sildenafil induced middle cerebral artery dilatation above therapeutic levels. In vivo, sildenafil dilated middle meningeal artery concomitant with a reduction in blood pressure. Tadalafil had no dilatory effects. PDE5 inhibitors show differential vascular activity in cerebral arteries from healthy animals; arterial dilatation is seen primarily above therapeutic levels. Such findings support clinical studies showing no vasodilator effects of sildenafil on cerebral arteries in healthy subjects. PMID: 22094063 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427221 Wed, 09 Nov 2011 05:00:00 +0100 5427221 http://www.medworm.com/index.php?rid=5427220&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%3D22094064%26dopt%3DAbstract Authors: Sundaram R, Naresh R, Ranadevan R, Shanthi P, Sachdanandam P Abstract Vitex negundo is a medicinal plant used to treat many ailments. An active compound of iridoid glucoside was isolated from V. negundo leaves and its efficacy was investigated in streptozotocin induced diabetic rats with special reference to carbohydrate metabolizing enzymes. The optimum dose of iridoid glucoside was determined by oral glucose tolerance test. The effects of iridoid glucoside were compared with glibenclamide Administration of iridoid glucoside (50mg/kg body weight) to diabetic rats for 30days resulted in significant reduction in the levels of plasma glucose, glycosylated hemoglobin and increase in the levels of insulin and hemoglobin. Administration of iridoid glucoside showed a significant... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427220 Wed, 09 Nov 2011 05:00:00 +0100 5427220 http://www.medworm.com/index.php?rid=5427218&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%3D22094066%26dopt%3DAbstract Authors: Hirata Y, Shimabukuro M, Uematsu E, Soeki T, Yamada H, Sakai Y, Nakayama M, Matsumoto K, Igarashi T, Sata M Abstract ONO-1301, a synthetic prostacyclin agonist with thromboxane synthase inhibitory activity, promotes the production of hepatocyte growth factor (HGF) and vascular endothelial growth factor (VEGF) by various cell types. Here, we evaluated the therapeutic efficacy of ONO-1301 in rats with ischemia/reperfusion injury. Ligation of the left anterior descending arteries was performed in 10-week-old Wistar rats, and released 30min later. A slow-release form of ONO-1301 was administered subcutaneously at 3h and 3weeks after reperfusion injury. Hemodynamic parameters were significantly improved in the ONO-1301 group. Histological analysis revealed that ONO-1301 suppres... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427218 Wed, 09 Nov 2011 05:00:00 +0100 5427218 http://www.medworm.com/index.php?rid=5427226&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%3D22085758%26dopt%3DAbstract Authors: Sawynok J, Reid AR Abstract The present study examined effects of caffeine on antinociception by acetaminophen in the formalin test in mice. It demonstrates that caffeine 10mg/kg inhibits antinociception produced by acetaminophen 300mg/kg i.p. against phase 2 flinches. Chronic administration of caffeine in the drinking water (0.1, 0.3g/l) for 8days also inhibits the action of acetaminophen. The selective adenosine A(1) receptor antagonist DPCPX 1mg/kg i.p. mimics the action of caffeine, but the selective adenosine A(2A) receptor antagonist SCH58261 3mg/kg i.p. does not. While acetaminophen produced the same effect in mice that were +/+, +/- and -/- for adenosine A(1) receptors, inhibition of antinociception by caffeine was seen only in +/+ and +/- mice. A higher dose of ca... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427226 Mon, 07 Nov 2011 05:00:00 +0100 5427226 http://www.medworm.com/index.php?rid=5427219&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%3D22094065%26dopt%3DAbstract In conclusion, argon enhanced ERK 1/2 activity in microglia via the upstream kinase MEK, probably through a direct mode of activation. ERK 1/2 signaling in astrocytes and neurons in vitro was also influenced, although not with statistical significance. Whether ERK 1/2 activation by argon affects cellular functions like differentiation and survival in the brain in vivo will have to be determined in future experiments. PMID: 22094065 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427219 Mon, 07 Nov 2011 05:00:00 +0100 5427219 http://www.medworm.com/index.php?rid=5427217&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%3D22094067%26dopt%3DAbstract Authors: Wu HJ, Hao J, Wang SQ, Jin BL, Chen XB Abstract To investigate the effects of Ligustrazine, a compound derived from chuanxiong, on tumor necrosis factor-α (TNF-α) stimulated endothelial cells. Human umbilical vein endothelial cells (HUVECs) were stimulated with TNF-α in vitro. Nitric oxide (NO) was measured as a standard of endothelial dysfunction. Two important indicators of autoimmunity, intracellular adhesion molecular-1 (ICAM-1) and heat shock protein 60 (HSP60), were selected to evaluate the influence of Ligustrazine on HUVECs. Ligustrazine (40μg/ml) significantly reversed the decrease in NO production induced by TNF-α (5ng/ml) in HUVECs. The expressions of ICAM-1 and HSP60 were increased by TNF-α treatment, but dramatically inhibited by treatment with ligustraz... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427217 Mon, 07 Nov 2011 05:00:00 +0100 5427217 http://www.medworm.com/index.php?rid=5427216&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%3D22094068%26dopt%3DAbstract Authors: da Silva Júnior ED, Caricati-Neto A, Jurkiewicz NH, Jurkiewicz A Abstract Because of the few studies that emphasize the in vivo use of amphetamine and ethanol, and their consequences on autonomic neurotransmission, we decided to study the effect of these drugs on peripheral noradrenergic neurotransmission of young animals. We used contractions of the vas deferens of adolescent rats as a model for the study of pre-treatment with both agents. The 30 to 40day old adolescent rats were pre-treated with amphetamine, at doses of 3mg/kg, or ethanol at doses of 1.2g/kg. Both agents were also used simultaneously to investigate possible interactions. The group treated with amphetamine showed a potentiation of the vas deferens contractions evoked by noradrenaline and barium (about 20... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427216 Mon, 07 Nov 2011 05:00:00 +0100 5427216 http://www.medworm.com/index.php?rid=5427228&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%3D22079424%26dopt%3DAbstract Authors: Gronwald C, Vegh V, Hollmann MW, Hahnenkamp A, Garaj V, Hahnenkamp K Abstract Development of postoperative hyperalgesia depends on N-methyl-d-aspartate (NMDA) receptor activation. Local anesthetics protect against those hyperalgesic pain states and inhibit NMDA receptor activation. To outline what structural features of local anesthetics are responsible for NMDA receptor inhibition we evaluated a series of experimental lidocaine analogs (carbanilic derivates). Human GluN1/GluN2A NMDA receptors were expressed recombinantly in Xenopus laevis oocytes. Peak currents were measured by voltage clamp technique. Oocytes were stimulated with glutamate/glycine (EC(50)). The responses following a 10min incubation with in total 13 experimental derivates of local anesthetics (10(-3)M-10... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427228 Fri, 04 Nov 2011 04:00:00 +0100 5427228 http://www.medworm.com/index.php?rid=5427227&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%3D22079770%26dopt%3DAbstract Authors: Yubero-Lahoz S, Ayestas MA, Blough B, Partilla JS, Rothman RB, de la Torre R, Baumann MH Abstract (±)-3,4-Methylenedioxymethamphetamine (MDMA) is an illicit drug that evokes transporter-mediated release of serotonin (5-HT) in the brain. 5-HT transporter (SERT) proteins are also expressed in non-neural tissues (e.g., blood), and evidence suggests that MDMA targets platelet SERT to increase plasma 5-HT. Here we tested two hypotheses related to the effects of MDMA on circulating 5-HT. First, to determine if MDMA metabolites might contribute to actions of the drug in vivo, we used in vitro microdialysis in rat blood specimens to examine the effects of MDMA and its metabolites on plasma 5-HT. Second, to determine whether effects of MDMA on plasma 5-HT might be used as an index... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5427227 Thu, 03 Nov 2011 04:00:00 +0100 5427227 http://www.medworm.com/index.php?rid=5267259&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%3D21867697%26dopt%3DAbstract This study examined the antinociceptive effects of two selective I(2) receptor ligands 2-BFI and BU224 (>2000-fold selectivity for I(2) receptors over α(2) adrenoceptors) in a hypertonic (5%) saline-induced writhing test and analyzed their interaction with morphine using a dose-addition analysis. Morphine, 2-BFI and BU224 but not agmatine produced a dose-dependent antinociceptive effect. Both composite additive curve analyses and isobolographical plots revealed a supra-additive interaction between morphine and 2-BFI or BU224, whereas the interaction between 2-BFI and BU224 was additive. The antinociceptive effect of 2-BFI and BU224 was attenuated by the I(2) receptor antagonist/α(2) adrenoceptor antagonist idazoxan but not by the selective α(2) adrenoceptor antagonist yohimbine, sugg... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267259 Fri, 30 Sep 2011 07:11:29 +0100 5267259 http://www.medworm.com/index.php?rid=5267258&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%3D21871878%26dopt%3DAbstract In this study, MCF-7/ADR cells, an adriamycin (ADR)-selected human breast tumor cell line with the MDR phenotype, were used to investigate the anticancer properties of this novel indirubin derivative. Cytotoxicity and apoptosis assays showed that PHII-7 significantly inhibited cell growth, induced apoptosis, potentiated ADR cytotoxicity and restored chemotherapy sensitivity in the MDR cancer cells. Further studies indicated that by down-regulation of P-gp expression, PHII-7 partially inhibited P-gp efflux pump function and increased intracellular accumulation of Rhodamine 123, a P-gp substrate. These results provide a biochemical basis for possible clinical application of PHII-7 alone or in combination with conventional antineoplastic agents in the treatment MDR tumors. PMID: 21871878 ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267258 Fri, 30 Sep 2011 07:11:20 +0100 5267258 http://www.medworm.com/index.php?rid=5267257&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%3D21871879%26dopt%3DAbstract Authors: Glick SD, Sell EM, McCallum SE, Maisonneuve IM Abstract 18-Methoxycoronaridine (18-MC), a putative anti-addictive agent, has been shown to decrease the self-administration of several drugs of abuse in rats. 18-MC is a potent antagonist at α3β4 nicotinic receptors. Consistent with high densities of α3β4 nicotinic receptors being located in the medial habenula and the interpeduncular nucleus, 18-MC has been shown to act in these regions to decrease both morphine and methamphetamine self-administration. The present study was conducted to determine if 18-MC's effect on nicotine self-administration is mediated by acting in these same brain regions. Because moderate densities of α3β4 receptors occur in the dorsolateral tegmentum, ventral tegmental area, and basolateral amy... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267257 Fri, 30 Sep 2011 07:11:11 +0100 5267257 http://www.medworm.com/index.php?rid=5267256&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%3D21871880%26dopt%3DAbstract Authors: Novotna A, Doricakova A, Vrzal R, Pavek P, Dvorak Z Abstract Cancer cell lines derived from hepatocytes have an altered phenotype and they lack hepatocyte-specific functions. It is at least partly due to the under-expression of transcription factors such as hepatocyte nuclear factor 4α (HNF4α), steroid receptor co-activator 1 (SRC1) etc. Recently, a strategy of transient transfection of human hepatic cells with HNF4α revealed improved hepatospecific functions, including the expression of drug-metabolizing enzymes. In the current study we established a human cell line derived from HepG2 cells stably transfected with human HNF4α, and we examined this line for hepatospecific markers. Of the 9 clones analyzed, we found an increased secretion of fibrinogen (9 clones), album... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267256 Fri, 30 Sep 2011 07:11:02 +0100 5267256 http://www.medworm.com/index.php?rid=5267255&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%3D21871881%26dopt%3DAbstract We examined the effects of EPA, especially to focus on nuclear factor kappa B (NF-κB), using Thy-1 nephritis models. Also the mechanism of EPA was investigated using small-interfering RNA (siRNA) in lipopolysaccharide (LPS)-stimulated proximal tubular epithelial cells (PTECs). In Thy-1 nephritis models, EPA significantly inhibited tubulointerstitial injury and the infiltration of macrophages into tubulointerstitial lesions except severe glomerular injury at early stage. Compared with control animals, NF-κB activation was significantly augmented in the Thy-1 nephritic kidney. However, treatment with EPA significantly reduced NF-κB activation, down-regulated the expressions of NF-κB-dependent molecules. Also in LPS-stimulated PTECs, LPS augmented NF-κB activation and the expression of N... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267255 Fri, 30 Sep 2011 07:10:53 +0100 5267255 http://www.medworm.com/index.php?rid=5267254&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%3D21871882%26dopt%3DAbstract Authors: Ndong C, O'Donnell D, Ahmad S, Groblewski T Abstract Comparison of human, rat and mouse cannabinoid CB(2) receptor primary sequences has shown significant divergence at the mRNA and protein sequence level, raising the possibility of species specific pharmacological properties. Additionally, given the importance of the dog as a non-rodent species for predicting human safety during the drug development process, we cloned the dog CB(2) receptor gene and characterized its in-vitro pharmacological properties in a recombinant expression system. A 1.1kb dog peripheral cannabinoid receptor (dCB(2)) fragment encoding a 360 amino acid protein was cloned from dog spleen cDNA. Analysis of the cloned dCB(2) polypeptide sequence revealed that it shares between 76 and 82% homology with r... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267254 Fri, 30 Sep 2011 07:10:45 +0100 5267254 http://www.medworm.com/index.php?rid=5267253&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%3D21871884%26dopt%3DAbstract Authors: Beberok A, Buszman E, Wrześniok D, Otręba M, Trzcionka J Abstract There have been described serious adverse events caused by ciprofloxacin in pigmented tissues. It is known that some fluoroquinolones bind well to melanin rich tissues, but the relation between their affinity to melanin and the skin or eye toxicity is not well documented. The aim of this study was to examine whether ciprofloxacin binds to melanin, and how this interaction affects the proliferation and melanization in melanocytes. We have demonstrated that complexes which ciprofloxacin forms with melanin possess at least two classes of independent binding sites. Their association constants are K(1)~10(5)M(-1) and K(2)~10(2)M(-1), respectively. Ciprofloxacin has induced evident concentration-dependent loss i... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267253 Fri, 30 Sep 2011 07:10:35 +0100 5267253 http://www.medworm.com/index.php?rid=5267252&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%3D21871885%26dopt%3DAbstract Authors: Mori A, Suzuki S, Sakamoto K, Nakahara T, Ishii K Abstract The large-conductance Ca(2+)-activated K(+) (BK(Ca)) channels modulate the retinal vascular tone, but question of whether the impairment of the channel function contributes to abnormalities of retinal circulation has not yet been completely elucidated. The purpose of this study was to examine effects of diabetes on the vasodilation induced by activation of BK(Ca) channels. Male Wistar rats were treated with streptozotocin and experiments were performed 2weeks later. The streptozotocin-treated animals were given drinking water containing 5% d-glucose to shorten the term in the development of retinal vascular dysfunction. The retinal vascular responses were assessed by measuring diameter of retinal arterioles in the ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267252 Fri, 30 Sep 2011 07:10:26 +0100 5267252 http://www.medworm.com/index.php?rid=5267251&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%3D21872583%26dopt%3DAbstract In this study, we investigated the cellular mechanism that is responsible for the vasodilator effect of curine in the rat aorta. The vasorelaxant activity of curine was recorded using a myograph. Ca(2+) currents in A7r5 cells were measured using the whole-cell patch-clamp technique. Intracellular Ca(2+) transients were determined using confocal microscopy. In a concentration-dependent manner, curine inhibited contractions elicited by high extracellular K(+) and Bay K8644 in the rat aorta and reduced the rise in the intracellular Ca(2+) concentration induced by membrane depolarization in response to an increase in extracellular K(+) concentration in vascular smooth muscle cells. Moreover, curine decreased the peak amplitude of L-type Ca(2+) currents (I(Ca,L)) in a concentration-dependent ma... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267251 Fri, 30 Sep 2011 07:10:09 +0100 5267251 http://www.medworm.com/index.php?rid=5267250&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%3D21872585%26dopt%3DAbstract Authors: Larsson AK, Hagfjärd A, Dahlén SE, Adner M Abstract Prostaglandin D(2) (PGD(2)), released through mast cell activation, is used as a non-invasive biomarker in patients with asthma. Since PGD(2) can elicit opposing effects on airway tone via activation of the PGD(2) receptors DP(1) and DP(2) as well as the thromboxane receptor TP, the aim of this study was to characterize the receptors that are activated by PGD(2) in the guinea pig lung parenchyma. PGD(2) and the thromboxane analog U46619 induced concentration-dependent contractions. U46619 was more potent and caused stronger effect than PGD(2). The specific TP receptor antagonist SQ-29548 and the combined TP and DP(2) receptor antagonist BAYu3405 concentration-dependently shifted the curves for both agonists to the right... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267250 Fri, 30 Sep 2011 07:09:49 +0100 5267250 http://www.medworm.com/index.php?rid=5267244&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%3D21946101%26dopt%3DAbstract Authors: Akimoto Y, Furuse M Abstract To clarify the mechanisms by which compound 48/80 (C48/80) induces scratching behavior, the involvement of dopamine D(1) receptors was investigated. The intracisternal (i.t.) administration of SCH23390 (1.0μg), a selective dopamine D(1) receptor antagonist, significantly decreased C48/80-induced scratching behavior in mice. These results suggest that dopamine D(1) receptors contribute to scratching behavior or the itch sensation induced by subcutaneous injection of C48/80 in mice. Co-administration of SCH23390 and C48/80 enhanced c-fos immunoreactivities in the peduncular part of the lateral hypothalamus (PLH), whereas the immunoreactivities in the other groups were unchanged. The dopaminergic system may be playing an important role in the sup... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267244 Wed, 21 Sep 2011 04:00:00 +0100 5267244 http://www.medworm.com/index.php?rid=5267243&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%3D21946102%26dopt%3DAbstract In conclusion, we showed that seizure activities were affected by pentoxifylline, H-89 and bucladesine via interactions with intracellular cAMP and cGMP signaling pathways, cyclic nucleotide-dependent protein kinases, and related neurotransmitters. PMID: 21946102 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267243 Wed, 21 Sep 2011 04:00:00 +0100 5267243 http://www.medworm.com/index.php?rid=5267242&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%3D21946103%26dopt%3DAbstract Authors: Ruiz MA, León DA, Albasanz JL, Martín M Abstract Adenosine plays an important neuroprotective role in brain, usually mediated by the activation of adenosine A(1) receptors. Prolonged activation of a G-protein-coupled receptor generally leads to the partial loss of the responsiveness of receptor-mediated transduction pathways (desensitization). Rat immature cortical neurons were treated with 100nM (-)N(6)-phenylisopropyladenosine (R-PIA), a selective A(1) receptor agonist, and the effect on adenosine A(1) receptor/adenylyl cyclase pathway was studied. Incubation with R-PIA for 6, 12, 24 and 48h elicited a time-dependent decrease in adenosine A(1) receptors in plasma membranes (92, 58, 43 and 26% of control, respectively), which was associated with variations in microsomal... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267242 Wed, 21 Sep 2011 04:00:00 +0100 5267242 http://www.medworm.com/index.php?rid=5267241&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%3D21946104%26dopt%3DAbstract This study was designed to evaluate the neuroprotective effects of α-ZAL, on the cultured differentiated PC-12 cells, while 17β-estradiol (17β-E2) has been used as an estrogen positive control. Following a 24h exposure of the cells to amyloid β-peptide fragment 25-35 (Aβ(25-35)), a significant reduction in cell survival and activities of total superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), as well as increased of malondialdehyde (MDA) were observed. However, preincubation of the cells with α-ZAL or 17β-E2 prior to Aβ(25-35) exposure elevated the cell survival and SOD and GSH-Px activities, and decreased the level of MDA. In addition, Aβ(25-35) caused a significant cell apoptosis and increased apoptotic rate, accompanied by decreasing of bcl-2 expression and increa... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267241 Wed, 21 Sep 2011 04:00:00 +0100 5267241 http://www.medworm.com/index.php?rid=5267240&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%3D21946105%26dopt%3DAbstract This study offers novel and mechanistic data to clarify molecular events that occur in the myocardium in doxorubicin-induced chronic cardiomyopathy. Doxorubicin led to a marked reduction/loss in dystrophin membrane localization in cardiomyocytes and left ventricular dysfunction, which might constitute, in association with sarcomeric actin/myosin proteins disruption, the structural basis of doxorubicin-induced cardiac depression. Moreover, increased sarcolemmal permeability suggests functional impairment of the dystrophin-glycoprotein complex in cardiac myofibers and/or oxidative damage. Increased expression of calpain, a calcium-dependent protease, was markedly increased in cardiomyocytes of doxorubicin-treated rats. Dantrolene improved survival rate and preserved myocardial dystrophin, ca... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267240 Wed, 21 Sep 2011 04:00:00 +0100 5267240 http://www.medworm.com/index.php?rid=5267239&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%3D21946106%26dopt%3DAbstract Authors: Lim H, Jin JH, Park H, Kim HP Abstract To identify anti-inflammatory flavonoid derivatives with optimal chemical structures, various 8-heterocyclic-substituted chrysin derivatives were previously synthesized and their effects on prostaglandin E(2) (PGE(2)) production from the lipopolysaccharide (LPS)-treated mouse macrophage cell line, RAW 264.7, were evaluated. Through this screening procedure, 5,7-dihydroxy-8-(pyridine-4yl)flavone (C-721) among the derivatives was selected for further pharmacological study. Contrary to the parent molecule, chrysin, C-721 was found to potently inhibit PGE(2) and NO production by LPS-treated RAW cells. The IC(50) values of C-721 were 6.2 and 22.6μM, respectively, for cyclooxygenase-2 (COX-2) mediated PGE(2) and inducible nitric oxide (iNO... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267239 Wed, 21 Sep 2011 04:00:00 +0100 5267239 http://www.medworm.com/index.php?rid=5267238&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%3D21946107%26dopt%3DAbstract Authors: Neto-Neves EM, Dias-Junior CA, Uzuelli JA, Pereira RP, Spiller F, Czaikoski PG, Tanus-Santos JE Abstract We investigated whether atorvastatin has beneficial hemodynamic effects during acute pulmonary thromboembolism (APT) and whether sildenafil improves these effects. We studied the involvement of oxidative stress, matrix metalloproteinases (MMPs), and neutrophil activation. APT was induced with autologous blood clots (500mg/kg) in anesthetized male lambs pretreated with atorvastatin (10mg/kg/day, subcutaneously; 1week) or vehicle (dimethyl sulfoxide 10% subcutaneously). Sildenafil (0.7mg/kg intravenously) or saline infusions were performed 60min after APT induction. Non-embolized control animals received saline. APT significantly increased pulmonary vascular resistance in... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267238 Wed, 21 Sep 2011 04:00:00 +0100 5267238 http://www.medworm.com/index.php?rid=5267236&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%3D21946109%26dopt%3DAbstract In this study we have investigated its duration of action in vitro in an effort to characterise the receptor and tissue components involved. Chinese hamster ovary cell membrane fragments were used to determine the kinetics of azelastine at the H(1) receptor in a radioligand binding assay. Further duration of action studies was completed in tissue preparations using guinea-pig trachea and human bronchus. In radioligand binding studies, azelastine reached steady state at the H(1) receptor after approximately 41min and exhibited a significantly slower dissociation rate constant from the receptor than the first generation antihistamine, diphenhydramine. In washout studies completed in guinea-pig and human airway in vitro tissue preparations, azelastine continued to antagonise the effects of hi... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267236 Wed, 21 Sep 2011 04:00:00 +0100 5267236 http://www.medworm.com/index.php?rid=5267235&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%3D21946110%26dopt%3DAbstract Authors: Kanimozhi G, Prasad NR, Ramachandran S, Pugalendi KV Abstract The purpose of this study was to investigate the antioxidant potential of umbelliferone, 7-hydroxy coumarin, and its role in the protection against radiation-induced oxidative damage in cultured human blood lymphocytes. It was found that the antioxidant effect of umbelliferone was dose dependent in hydroxyl (OH(•)), superoxide anion (O(2)(•-)), 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid radical cation (ABTS(•+)) and 1,1-diphenyl-2-picrylhydrazyl (DPPH(•)) radical scavenging assays. To explore the radioprotective effect of umbelliferone, freshly isolated human blood lymphocytes were treated with 124μM umbelliferone (optimum dose-fixed by MTT assay) 30min before 3Gy irradiation. It was found th... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267235 Wed, 21 Sep 2011 04:00:00 +0100 5267235 http://www.medworm.com/index.php?rid=5267234&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%3D21946111%26dopt%3DAbstract Authors: Tain YL, Hsu CN, Lin CY, Huang LT, Lau YT Abstract Asymmetric dimethylarginine (ADMA), an endogenous inhibitor of NOS, decreases NO synthesis. Plasma ADMA concentrations increase markedly in hypertension. We tested whether the development of hypertension and the increases in ADMA in spontaneously hypertensive rats (SHR) are prevented by aliskiren, a renin inhibitor. Male SHRs and normotensive Wistar Kyoto (WKY) control rats, aged 4weeks (pre-hypertensive stage), were assigned to 4 groups: untreated SHRs and WKY rats, and SHRs that received oral aliskiren 10 and 30mg/kg/day for 6weeks. All rats were sacrificed at age 10weeks. Blood pressure decreased at age 6, 8, and 10weeks in SHRs that received high-dose aliskiren. Aliskiren mitigated the increases in plasma ADMA in SHRs.... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267234 Wed, 21 Sep 2011 04:00:00 +0100 5267234 http://www.medworm.com/index.php?rid=5267233&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%3D21946112%26dopt%3DAbstract The objective of the present study was to evaluate the effects of a selective mGlu5 receptors antagonist-MTEP, and mGlu1 receptors antagonist-EMQMCM, on two processes relevant to alcohol addiction: the expression of ethanol-induced conditioned place preference (CPP) paradigm, and ethanol withdrawal audiogenic seizures in rats. Our experiments indicated that EMQMCM at the doses of 5 and 10mg/kg, and MTEP at the doses of 2.5 and 5mg/kg, significantly attenuated the expression of ethanol CPP. Furthermore, both group I mGlu receptor antagonists, i.e. EMQMCM at the dose of 10mg/kg and MTEP at the dose of 5mg/kg, attenuated audiogenic seizures induced by the sound stimulus 12h after withdrawal of ethanol in dependent rats. Our study shows the importance of mGlu5 and mGlu1 receptors for the expre... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267233 Wed, 21 Sep 2011 04:00:00 +0100 5267233 http://www.medworm.com/index.php?rid=5267226&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%3D21946113%26dopt%3DAbstract Authors: Gardoni F, Zianni E, Eramo A, Canonico LP, Di Luca M Abstract In the last decade, several neuroprotective therapies have been proposed for Parkinson's disease and rasagiline was indicated as one of the most promising candidates by preclinical studies. The drug has already been tested in phase III clinical studies (the ADAGIO study). The mechanism underlying rasagiline-dependent neuroprotection is complex and almost unknown. Here, we show that rasagiline is involved in the regulation of the molecular composition of the postsynaptic density of glutamatergic synapses. In hippocampus as well as in striatum, rasagiline induces a significant reduction of synaptic levels of NR2A-containing NMDA receptors and in hippocampal slices it also significantly decreases synaptic levels of... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267226 Wed, 21 Sep 2011 04:00:00 +0100 5267226 http://www.medworm.com/index.php?rid=5267225&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%3D21946114%26dopt%3DAbstract In this study, we show that PCA can promote the neuronal differentiation combined with fetal bovine serum (FBS) in vitro, although it cannot initiate the differentiation of NS/PCs by itself. Moreover, PCA is able to induce neuronal maturation and efficiently promote neurite outgrowth. On the other hand, PCA facilitates survival of phenotypes differentiated from cultured NS/PCs, which was associated with an increased percentage of the cellular viability and a decreased percentage of cells undergoing apoptosis under differentiation conditions. In addition, PCA-induced survival is also mediated with the activating of endogenous antioxidant enzymes. These results suggest that PCA may serve as a useful reference for future studies in designing stem cell strategies to promote brain recovery and ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267225 Wed, 21 Sep 2011 04:00:00 +0100 5267225 http://www.medworm.com/index.php?rid=5267224&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%3D21946115%26dopt%3DAbstract Authors: Spaccapelo L, Bitto A, Galantucci M, Ottani A, Irrera N, Minutoli L, Altavilla D, Novellino E, Grieco P, Zaffe D, Squadrito F, Giuliani D, Guarini S Abstract Indirect evidence indicates that, in cerebral ischemia, melanocortins have neuroprotective effects likely mediated by MC(4) receptors. To gain direct insight into the role of melanocortin MC(4) receptors in ischemic stroke, we investigated the effects of a highly selective MC(4) receptor agonist. Gerbils were subjected to transient global cerebral ischemia by occluding both common carotid arteries for 10min. In saline-treated stroke animals, an impairment in learning and memory occurred that, at day 11 after stroke, was associated with hippocampus up-regulation of tumor necrosis factor-α (TNF-α), BAX, activated extr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267224 Wed, 21 Sep 2011 04:00:00 +0100 5267224 http://www.medworm.com/index.php?rid=5267223&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%3D21946116%26dopt%3DAbstract Authors: Hosseinmardi N, Azimi L, Fathollahi Y, Javan M, Naghdi N Abstract Effects of morphine on synaptic transmission and plasticity in the hippocampus area CA1 following in vivo sodium salicylate and the potential molecular mechanism were investigated. Population spikes (PS) were recorded from stratum pylamidale of area CA1 following stimulation of Schaffer collaterals in slices taken from control and sodium salicylate injected rats. To induce long term potentiation (LTP), a 100Hz tetanic stimulation was used. Acute in vitro morphine increased baseline PS amplitude in control slices but not in slices taken from sodium salicylate treated rats. In vivo chronic salicylate did slightly decrease and/or destabilize LTP of CA1 synaptic transmission. We also found that mRNA of NR2A subu... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267223 Wed, 21 Sep 2011 04:00:00 +0100 5267223 http://www.medworm.com/index.php?rid=5267222&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%3D21951963%26dopt%3DAbstract Authors: Zhou LL, Lin ZX, Fung KP, Cheng CH, Che CT, Zhao M, Wu SH, Zuo Z Abstract Psoriasis is a chronic inflammatory skin disease affecting 1-3% of the world's population. Traditional Chinese medicines have been extensively used for treating psoriasis with promising clinical results. Celastrol, a triterpenoid isolated from a Chinese herb Celastrus orbiculatus caulis, has been known to have diverse pharmacological effects such as anti-inflammatory, anti-cancer and antioxidant activities. The present study aimed at evaluating the anti-proliferative action of celastrol on cultured HaCaT cells and elucidating the mechanisms of action involved. Celastrol was shown to inhibit HaCaT cells growth with an IC(50) value of 1.1μM as measured by MTT assay. The ability of celastrol to induce ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267222 Wed, 21 Sep 2011 04:00:00 +0100 5267222 http://www.medworm.com/index.php?rid=5267221&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%3D21951964%26dopt%3DAbstract In conclusion, our study showed that acute myocardial ischemia can directly upregulate BNP expression at the translational and transcriptional levels through the action of il-6, and this process is associated with the upregulation of TGF-β1/Smad2 signal path. PMID: 21951964 [PubMed - as supplied by publisher] (Source: European Journal of Pharmacology) European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267221 Wed, 21 Sep 2011 04:00:00 +0100 5267221 http://www.medworm.com/index.php?rid=5267220&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%3D21951965%26dopt%3DAbstract Authors: Bie B, Zhao ZQ Abstract The neuropeptide substance P is synthesized in a proportion of neurons of the peripheral and central nervous system, and the receptor for substance P, tachykinin NK(1) receptor, has been identified in numerous areas of the central nervous system including the spinal cord. The present investigation was to confirm the existence of tachykinin NK(1) receptor on rat dorsal root ganglion (DRG) neurons and characterize the adaptation of inward current evoked by substance P during carrageenan-induced peripheral inflammation. Using whole-cell voltage recording technique, our results demonstrated that 1μM substance P elicited significant inward current in a small population of small-diameter DRG neurons of control rats (7%, n=218) and in a bigger proportion ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267220 Wed, 21 Sep 2011 04:00:00 +0100 5267220 http://www.medworm.com/index.php?rid=5267219&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%3D21951966%26dopt%3DAbstract Authors: Ueda T, Ugawa S, Ishida Y, Shimada S Abstract Aripiprazole has made a significant contribution to the treatment of schizophrenia and related disorders. It has improved its safety and tolerability profiles, and these effects have been attributed to its pharmacological profile at the serotonin 5-HT and dopamine D(2) receptors. To discover compounds that have a similar pharmacological profile, we introduced a generic single-cell-based calcium imaging assay that standardizes the readouts from various assays used in previous studies on aripiprazole. In the present assay, the efficacy and potency of known ligands of serotonin 5-HT(1A), 5-HT(2A), 5-HT(2C), 5-HT(7) and dopamine D(2L) receptors were comparable to those found in previous studies using a variety of readouts. The deve... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267219 Wed, 21 Sep 2011 04:00:00 +0100 5267219 http://www.medworm.com/index.php?rid=5267218&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%3D21951967%26dopt%3DAbstract Authors: Himaya SW, Bomi R, Zhong-Ji Q, Li Y, Kim SK Abstract Unregulated activation of microglia is a key risk factor contributes to neurodegenerative diseases and suppression of this phenomenon is considered as a potential therapeutic target. The compound isolated from sea horse Hippocampus kuda Bleeler; 1-(5-bromo-2-hydroxy-4-methoxyphenyl)ethanone [SE1] was characterized for its ability in suppressing LPS mediated activation of murine BV-2 cells. Despite the presence of various active molecular groups in the structure, SE1 has not well explored for its biological activities. The outcome of this study clearly indicated that SE1 inhibited the production of inflammatory mediators; nitric oxide, prostaglandin E(2) and pro-inflammatory cytokines. Furthermore, it inhibited the protei... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267218 Wed, 21 Sep 2011 04:00:00 +0100 5267218 http://www.medworm.com/index.php?rid=5267217&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%3D21951968%26dopt%3DAbstract Authors: Yang K, Takeuchi K, Wei F, Dubner R, Ren K Abstract The interaction between the group I metabotropic glutamate (mGlu) receptors and N-methyl-D-aspartate (NMDA) receptors plays a critical role in spinal hyperexcitability and hyperalgesia. The cellular mechanisms underlying this interaction remain unknown. Utilizing an ex vivo spinal slice preparation from young adult rats, we investigated the group I mGlu receptor modulation of NMDA receptor-mediated current in superficial dorsal horn neurons by patch clamp recording after complete Freund's adjuvant (CFA)-induced hind paw inflammation. We show that NMDA receptor-mediated dorsal root stimulation-evoked EPSC (eEPSC) and NMDA-induced current was enhanced in the inflamed rats, compared to naïve rats and this effect was attenua... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267217 Wed, 21 Sep 2011 04:00:00 +0100 5267217 http://www.medworm.com/index.php?rid=5267216&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%3D21951969%26dopt%3DAbstract Authors: Parveen S, Sahoo SK Abstract Polymeric nanoparticles have long been sought after as carriers for systemic and targeted drug delivery. The ability of these particles to circulate in the bloodstream for a prolonged period of time is often a prerequisite for successful targeted delivery. To achieve this, paclitaxel loaded chitosan and polyethylene glycol coated PLGA (PLGA-CS-PEG) nanoparticles were formulated and characterized that could efficiently encapsulate hydrophobic drugs, and also evade the phagocytic uptake by reducing opsonization by blood proteins, hence increasing the bioavailability of the drug. In our study, we primarily assessed a rational approach for designing and formulating ideal long-circulating nanoparticles by optimizing the concentration of chitosan (CS... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267216 Wed, 21 Sep 2011 04:00:00 +0100 5267216 http://www.medworm.com/index.php?rid=5267237&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%3D21946108%26dopt%3DAbstract Authors: Bundhoo SS, Anderson RA, Sagan E, Hassan N, Pinder AG, Rogers SC, Morris K, James PE Abstract Thienopyridines (ticlopidine, clopidogrel and prasugrel) are pro-drugs that require metabolism to exhibit a critical thiol group in the active form that binds to the P2Y(12) receptor to inhibit platelet activation and prevent thrombus formation in vivo. We investigated whether these thienopyridines participate in S-nitrosation (SNO) reactions that might exhibit direct anti-platelet behaviour. Optimum conditions for in vitro formation of thienopyridine-SNO formation were studied by crushing ticlopidine, clopidogrel or prasugrel into aqueous solution and adding sodium nitrite, or albumin-SNO. Ozone-based chemiluminescence techniques were utilised to specifically detect NO release fr... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267237 Mon, 19 Sep 2011 04:00:00 +0100 5267237 http://www.medworm.com/index.php?rid=5267247&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%3D21944925%26dopt%3DAbstract In this study, we demonstrated that GL-V9 inhibited cells growth via inducing apoptosis and G2/M cell cycle arrest in human hepatocellular carcinoma HepG2 cells. Following the treatment of HepG2 cells with GL-V9, we observed poly (ADP-ribose) polymerase (PARP) cleavage and activation of caspase-3 and caspase-9, while caspase-8 remained unchanged. The expression ratio of Bcl-2/Bax was also decreased in GL-V9-treated cells. Meanwhile, the cell cycle-related proteins, such as cyclin B1, CDK1 and cdc25 were down-regulated in GL-V9-induced G2/M cell cycle arrest. Furthermore, we showed that GL-V9-induced apoptosis in HepG2 cells was achieved through mitochondrial pathway. It also regulated changes of mitochondrial membrane potential and increased the production of intracellular reactive oxygen ... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267247 Sat, 17 Sep 2011 04:00:00 +0100 5267247 http://www.medworm.com/index.php?rid=5267246&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%3D21944926%26dopt%3DAbstract Authors: Holtman JR, Dwoskin LP, Dowell C, Wala EP, Zhang Z, Crooks PA, McIntosh JM Abstract Chronic pain is inadequately managed with currently available classes of analgesic drugs. Recently, peptide antagonists of the α9α10 nicotinic acetylcholine receptor were shown to be analgesic. The present study was conducted to characterize a novel small molecule, non-peptide antagonist at nicotinic receptors. The tetrakis-quaternary ammonium compound ZZ-204G was evaluated for functional activity on cloned nicotinic receptors expressed in Xenopus oocytes. In-vivo efficacy was assessed in rat models of tonic inflammatory pain (formalin test), neuropathic pain (chronic constriction nerve injury), and thermal nociception (tail flick test). ZZ-204G was an antagonist at nicotinic receptors in... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267246 Sat, 17 Sep 2011 04:00:00 +0100 5267246 http://www.medworm.com/index.php?rid=5267261&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%3D21937012%26dopt%3DAbstract Authors: Saravana Kumar M, Raja B Abstract The present study was undertaken to assess the antihypertensive and antioxidant effects of veratric acid on N(ω)-nitro-L arginine methyl ester (l-NAME) induced hypertensive rats. Hypertension was induced in adult male albino rats of the Wistar strain, weighing 180-220g, by oral administration of the l-NAME (40mg/kg body weight/day) in drinking water for 4weeks. Rats were treated with various doses of veratric acid (20, 40, 80mg/kg/day) for four weeks. Hypertension was manifested by considerably increased systolic and diastolic blood pressure and the toxic effect of l-NAME was determined using lipid peroxidative markers (thiobarbituric acid reactive substances and lipid hydroperoxides). We also assessed the activities of enzymatic antioxid... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267261 Fri, 16 Sep 2011 04:00:00 +0100 5267261 http://www.medworm.com/index.php?rid=5267249&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%3D21933671%26dopt%3DAbstract Authors: Fujiwara Y, Tsuchiya H, Sakai N, Shibata K, Fujimura A, Koshimizu TA Abstract Effective detection of potential nephrotoxicity is crucial for pre-clinical drug development. We evaluated a sensitive animal model for drug-induced kidney injury, which includes hemi-nephrectomy of mice. Although bucillamine and d-penicillamine are used for the treatment of rheumatoid arthritis in Japan, drug-related adverse effects on the kidney can limit their therapeutic utilities. When bucillamine (1000 or 2000mg/kg/day) or d-penicillamine (2000mg/kg/day) were orally administered to hemi-nephrectomised BALB/c mice, the urinary protein levels of bucillamine-treated mice, but not of those treated with d-penicillamine, the vehicle, or in bucillamine treated unnephrectomized mice, were significa... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267249 Fri, 16 Sep 2011 04:00:00 +0100 5267249 http://www.medworm.com/index.php?rid=5267265&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%3D21930119%26dopt%3DAbstract Authors: Nazary M, der Zee HV, Prens E, Folkerts G, Boer J Abstract The focus of this review is to discuss the pathogenesis and the pharmacotherapy of Hidradenitis suppurativa (HS). HS is a distressing chronic skin disorder characterized by abscesses, boils, fistulas and scarring, generally affecting the groins, anogenital area and axillae. It is a common disease with an estimated prevalence of 1%. The etiology is unknown. HS was thought to be a disease of the apocrine sweat glands, but histological findings indicate that HS is a disease arising from the hair follicles. Several pathogenic factors seem important including genetic predisposition, smoking, obesity and an aberrant immune response to commensal flora. The management of HS is tremendously challenging because effective the... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267265 Wed, 14 Sep 2011 04:00:00 +0100 5267265 http://www.medworm.com/index.php?rid=5267264&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%3D21930120%26dopt%3DAbstract Authors: Fouad AA, Jresat I Abstract The therapeutic potential of cannabidiol, the major non-psychotropic Cannabis constituent, was investigated in rats exposed to ischemia/reperfusion liver injury. Ischemia was induced by clamping the pedicle of the left hepatic lobe for 30min, and cannabidiol (5mg/kg, i.v.) was given 1h following the procedure and every 24h thereafter for 2days. Ischemia/reperfusion caused significant elevations of serum alanine aminotransferase and hepatic malondialdehyde, tumor necrosis factor-α and nitric oxide levels, associated with significant decrease in hepatic reduced glutathione. Cannabidiol significantly attenuated the deterioration in the measured biochemical parameters mediated by ischemia/reperfusion. Histopathological examination showed that canna... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267264 Wed, 14 Sep 2011 04:00:00 +0100 5267264 http://www.medworm.com/index.php?rid=5267263&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%3D21930121%26dopt%3DAbstract Authors: Khundakar A, Zetterström T Abstract Brain-derived neurotrophic factor (BDNF) has been suggested as a target for antidepressant treatment and chronic antidepressant drug administration shows a 'biphasic effect' on BDNF mRNA in rat hippocampus (transient decrease followed by an increase). In comparison, following acute administration only, an inhibitory action on BDNF gene expression is detected. The present study aimed to understand the mechanism behind the acute inhibitory action on BDNF gene expression by investigating the possible involvement of γ-aminobutyric acid (GABA) receptors in mediating this effect. Rats were injected with either saline, the GABA(A) selective compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP), the benzodiazepine flunitrazepam or the... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267263 Wed, 14 Sep 2011 04:00:00 +0100 5267263 http://www.medworm.com/index.php?rid=5267262&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%3D21930122%26dopt%3DAbstract Authors: Kong F, Xu L, He D, Zhang X, Lu H Abstract A maternal fetal rat model was developed to study the effects of gestational isoflurane exposure on postnatal memory and learning and investigate the potential mechanisms. Pregnant rats at gestational day 14 were exposed to 1.3% isoflurane for 4h. Spatial learning and memory of the offspring were examined using the Morris Water Maze. The expression levels of C/EBP homologous transcription factor protein (CHOP) and caspase-12 in the hippocampus of the pups were determined by immunohistochemistry and western blot analysis. Simultaneously, the ultrastructure changes of synapse in the hippocampal CA1 and dentate gyrus region were also observed by transmission electron microscopy (TEM). Prenatal exposure to isoflurane impaired postnata... European Journal of Pharmacology journals http://www.medworm.com/rss/comments.php?id=5267262 Wed, 14 Sep 2011 04:00:00 +0100 5267262