British Journal of PharmacologyThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. Subscribe to this data using MyMedWorm.Subscribe to this data using GoogleReader.Subscribe to this data using Bloglines.Subscribe to this data using MyYahoo.

This page shows you the latest items in this publication.

Pages: 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28

1389 records returned

Pharmacokinetics and pharmacodynamics of a new reformulated microemulsion and the long-chain triglyceride emulsion of propofol in beagle dogsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Microemulsion propofol was pharmacodynamically bioequivalent to LCT propofol although pharmacokinetic bioequivalence was incomplete, and demonstrated linear pharmacokinetics at the applied dose ranges. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 20, 2009 Category: Drugs & Pharmacology Authors: S-H Lee, J-L Ghim, M-H Song, H-G Choi, B-M Choi, H-M Lee, E-K Lee, Y-J Roh, G-J Noh Source Type: journals

Therapeutic potential for novel drugs targeting the type 1 cholecystokinin receptorEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cholecystokinin (CCK) is a physiologically important gastrointestinal and neuronal peptide hormone, with roles in stimulating gallbladder contraction, pancreatic secretion, gastrointestinal motility and satiety. CCK exerts its effects via interactions with two structurally related class I guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs), the CCK1 receptor and the CCK2 receptor. Here, we focus on the CCK1 receptor, with particular relevance to the broad spectrum of signalling initiated by activation with the natural full agonist peptide ligand, CCK. Distinct ligand-binding pockets have been defined f...
Source: British Journal of Pharmacology - November 19, 2009 Category: Drugs & Pharmacology Authors: Erin E Cawston, Laurence J Miller Source Type: journals

Phe369(7.38) at human 5-HT7 receptors confers interspecies selectivity to antagonists and partial agonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: We propose that the interspecies difference in binding affinities observed for the compounds at human and rat 5-HT7 receptors is due to the nature of the residue at position 7.38. Our molecular modelling simulations suggest that Phe(7.38) in the human receptor is integrated in the hydrophobic pocket in the central part of the binding site [Phe(6.51)-Phe(6.52)] and allows a tighter binding of the ligands when compared with the rat receptor. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 18, 2009 Category: Drugs & Pharmacology Authors: Thibault Varin, Hugo Gutiérrez-de-Terán, Marián Castro, José Brea, Frederic Fabis, François Dauphin, Johan Åqvist, Pilar Perez, Javier Burgueño, José Miguel Vela, Maria Isabel Loza, Jordi Rodrigo Source Type: journals

The thorough QT/QTc study 4 years after the implementation of the ICH E14 guidanceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The ICH E14 guidance on how to clinically assess a new drug's liability to prolong the QT interval was adopted in May 2005. A centre-piece of the guidance was the establishment of one single trial, the 'thorough QT/QTcstudy', intended to confidently identify drugs that may cause QT prolongation. Initially perceived as a great challenge, this study has rapidly become a standard component of all clinical development programs for new molecular entities. The study is normally conducted in healthy volunteers, includes both a positive and a negative (placebo) control and is stringently powered to exclude an effect on the QTc int...
Source: British Journal of Pharmacology - November 18, 2009 Category: Drugs & Pharmacology Authors: B Darpo Source Type: journals

The benzoxathiolone LYR-71 down-regulates interferon-γ-inducible pro-inflammatory genes by uncoupling tyrosine phosphorylation of STAT-1 in macrophagesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Taken together, LYR-71 could restrain IFN-[gamma]-induced inflammatory responses through uncoupling the tyrosine phosphorylation of STAT-1, an activation index of JAK[ndash]STAT-1 signalling, in macrophages. These results may provide a molecular mechanism underlying anti-inflammatory actions shown by benzoxathiolone derivatives. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 18, 2009 Category: Drugs & Pharmacology Authors: E-Y Chung, B-H Kim, I-J Lee, E Roh, S-J Oh, J-A Kwak, Y-R Lee, B Ahn, S-Y Nam, S-B Han, Y Kim Source Type: journals

Characterization of biosynthesis and modes of action of prostaglandin E2 and prostacyclin in guinea pig mesenteric lymphatic vesselsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Our findings characterized the inhibition of lymphatic pumping induced by PGE2 or prostacyclin in guinea pig mesenteric lymphatics. This action is likely to impair oedema resolution and to contribute to the pro-inflammatory actions of these prostaglandins. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 17, 2009 Category: Drugs & Pharmacology Authors: Sonia Rehal, Pauline Blanckaert, Simon Roizes, Pierre-Yves von der Weid Source Type: journals

Berry anthocyanins and anthocyanidins exhibit distinct affinities for the efflux transporters BCRP and MDR1Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Although the anthocyanidins under study may alter pharmacokinetics of drugs that are BCRP substrates, they are less likely to interfere with activities of MDR1 substrates. The present data suggest that several anthocyanins and anthocyanidins may be actively transported out of intestinal tissues and endothelia, limiting their bioavailability in plasma and brain. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 17, 2009 Category: Drugs & Pharmacology Authors: A Dreiseitel, B Oosterhuis, KV Vukman, P Schreier, A Oehme, S Locher, G Hajak, PG Sand Source Type: journals

[6S]-5-methyltetrahydrofolate increases plasma folate more effectively than folic acid in women with the homozygous or wild-type 677C→T polymorphism of methylenetetrahydrofolate reductaseEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These data suggest that [6S]-5-MTHF increases plasma folate more effectively than FA irrespective of the 677C[rarr]T mutation of the MTHFR. This natural form of folate could be an alternative to FA supplementation or fortification. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 17, 2009 Category: Drugs & Pharmacology Authors: R Prinz-Langenohl, S Brämswig, O Tobolski, YM Smulders, DEC Smith, PM Finglas, K Pietrzik Source Type: journals

Dual effect of the novel peptide antagonist K-14585 on proteinase-activated receptor-2-mediated signallingEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These data reveal that K-14585 has a duality of action functioning both as an antagonist and agonist due to either partial agonist actions or possible agonist-directed signalling. The data also suggest two modes of p38 MAP kinase activation emanating from PAR2, one Gq/11-dependent and the other Gq/11-independent. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 16, 2009 Category: Drugs & Pharmacology Authors: Fui Goon Goh, Pei Yuen Ng, Mary Nilsson, Toru Kanke, Robin Plevin Source Type: journals

Rosiglitazone via upregulation of Akt/eNOS pathways attenuates dysfunction of endothelial progenitor cells, induced by advanced glycation end productsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: The PPAR[gamma] agonist rosiglitazone increased EPC function and attenuated EPC dysfunction induced by AGEs via upregulating the Akt-eNOS signal pathways of EPCs. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 16, 2009 Category: Drugs & Pharmacology Authors: Chun Liang, Yusheng Ren, Hongbin Tan, Zhiqing He, Qijun Jiang, Jianxiang Wu, Yi Zhen, Min Fan, Zonggui Wu Source Type: journals

Dalcetrapib: no off-target toxicity on blood pressure or on genes related to the renin-angiotensin-aldosterone system in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: In contrast to torcetrapib, dalcetrapib did not increase blood pressure or RAAS-related gene expression in rats, suggesting that the off-target effects of torcetrapib are not a common feature of all compounds acting on cholesteryl ester transfer protein. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 16, 2009 Category: Drugs & Pharmacology Authors: ESG Stroes, JJP Kastelein, A Bénardeau, O Kuhlmann, D Blum, LA Campos, RG Clerc, EJ Niesor Source Type: journals

Potentiation by WIN 55,212-2 of GABA-activated currents in rat trigeminal ganglion neuronesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: The potentiation by WIN 55,212-2 of IGABA in primary sensory neurones may help to elucidate the mechanism underlying the modulation of analgesia by cannabinoids in the spinal dorsal horn. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 16, 2009 Category: Drugs & Pharmacology Authors: Zhi-Wang Li, Jian Zhang, Chang-han Ouyang, Chao-Ying Li, Feng-Bo Zhao, Yu-Wei Liu, Yong-Xun Ai, Wang-Ping Hu Source Type: journals

Hydrogen peroxide affects contractile activity and anti-oxidant enzymes in rat uterusEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: H2O2 induced dose-dependent relaxation of isolated rat uteri mainly via changes in voltage-dependent potassium channels. Decreasing generation of reactive oxygen species by stimulation of anti-oxidative pathways may lead to new approaches to the management of dysfunctional uteri. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 16, 2009 Category: Drugs & Pharmacology Authors: I Appiah, S Milovanovic, R Radojicic, A Nikolic-Kokic, Z Orescanin-Dusic, M Slavic, S Trbojevic, R Skrbic, MB Spasic, D Blagojevic Source Type: journals

Cardiovascular changes in spontaneously hypertensive rats are improved by chronic treatment with zofenoprilEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Antihypertensive effects of chronic treatment with zofenopril were accompanied by recovery of endothelial function and improvement of cardiovascular structure. Low-dose zofenopril had little effect on blood pressure, with some benefits on cardiovascular structure and function. Inhibition of ACE and antioxidant activity were involved in these effects. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 16, 2009 Category: Drugs & Pharmacology Authors: M Gómez-Roso, MJ Montero, R Carrón, MA Sevilla Source Type: journals

The impact of GPCR structures on pharmacology and structure-based drug designEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
After many years of effort, recent technical breakthroughs have enabled the X-ray crystal structures of three G-protein-coupled receptors (GPCRs) ([beta]1 and [beta]2 adrenergic and adenosine A2a) to be solved in addition to rhodopsin. GPCRs, like other membrane proteins, have lagged behind soluble drug targets such as kinases and proteases in the number of structures available and the level of understanding of these targets and their interaction with drugs. The availability of increasing numbers of structures of GPCRs is set to greatly increase our understanding of some of the key issues in GPCR biology. In particular, wh...
Source: British Journal of Pharmacology - November 14, 2009 Category: Drugs & Pharmacology Authors: Miles Congreve, Fiona Marshall Source Type: journals

Thalidomide attenuates nitric oxide-driven angiogenesis by interacting with soluble guanylyl cyclaseEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion and implications: Our results showed that thalidomide interacted with sGC, suppressing cGMP levels in endothelial cells, thus exerting its anti-angiogenic effects. These results could lead to the formulation of thalidomide-based drugs to curb angiogenesis by targeting sGC. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 13, 2009 Category: Drugs & Pharmacology Authors: Syamantak Majumder, Megha Rajaram, Ajit Muley, Himabindu S Reddy, KP Tamilarasan, Gopi Krishna Kolluru, Swaraj Sinha, Jamila H Siamwala, Ravi Gupta, R Ilavarasan, S Venkataraman, KC Sivakumar, Sharmila Anishetty, Pradeep G Kumar, Suvro Chatterjee Source Type: journals

Epigallocatechin gallate reduces human monocyte mobility and adhesion in vitroEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Under our experimental conditions, EGCG treatment inhibited the migration and adhesion of monocytes. These inhibitory effects of EGCG on monocyte function should be considered as a promising new anti-inflammatory response with a potential therapeutic role in the treatment of inflammation-dependent diseases. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 13, 2009 Category: Drugs & Pharmacology Authors: Esther Melgarejo, Miguel Ángel Medina, Francisca Sánchez-Jiménez, José Luis Urdiales Source Type: journals

U-shaped dose-dependent effects of BmK AS, a unique scorpion polypeptide toxin, on voltage-gated sodium channelsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: BmK AS modulated the VGSCs in a unique U-shaped dose-dependent manner, which could be due to the opposing effects of binding to two distinct receptor sites on the VGSCs. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 13, 2009 Category: Drugs & Pharmacology Authors: Mang-Mang Zhu, Jie Tao, Miao Tan, Hong-tian Yang, Yong-Hua Ji Source Type: journals

Glucocorticoid-stimulated, transcription-independent release of annexin A1 by cochlear Hensen cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These findings suggest that ANXA1 could be a major mediator of the anti-inflammatory effects of glucocorticoids in the cochlea and identify new molecular targets for prevention of sudden sensorineural hearing loss. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 13, 2009 Category: Drugs & Pharmacology Authors: F Kalinec, P Webster, A Maricle, D Guerrero, DN Chakravarti, B Chakravarti, R Gellibolian, G Kalinec Source Type: journals

Differential inhibitory effects of drugs acting at the noradrenaline and 5-hydroxytrptamine transporters in rat and human neocortical synaptosomesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: This study provides the first compilation of drug potency at native human neocortical SERT and NET. The significant species differences (viz., human vs. rat) in drug potency suggest that the general use of rodent data should be limited to predict clinical efficacy or profile. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 13, 2009 Category: Drugs & Pharmacology Authors: M Mantovani, DJ Dooley, A Weyerbrock, R Jackisch, TJ Feuerstein Source Type: journals

Platelet aggregation responses are critically regulated in vivo by endogenous nitric oxide but not by endothelial nitric oxide synthaseEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Platelets are regulated by endogenous NO in vivo, primarily by NO originating from the environment external to the platelet with a negligible or undetectable role of platelet-derived NO. Raised levels of endogenous NOS inhibitors, as reported in a range of diseases were not, in isolation, sufficient to enhance platelet activity and NOS-3 is not essential for normal platelet function in vivo due to the presence of bioactive NO following deletion of NOS-3. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 12, 2009 Category: Drugs & Pharmacology Authors: C Tymvios, C Moore, S Jones, A Solomon, D Sanz-Rosa, M Emerson Source Type: journals

β2-Adrenoceptors and non-β-adrenoceptors mediate effects of BRL37344 and clenbuterol on glucose uptake in soleus muscle: studies using knockout miceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Ten nM BRL37344 and 100 nM clenbuterol have opposite effects on glucose uptake but both effects are mediated by the [beta]2-adrenoceptor [ndash] apparently an example of agonist-directed signalling. Ten pM BRL37344, 10 pM clenbuterol and 100 nM clenbuterol in the presence of ICI118551 stimulate glucose uptake via [beta]-adrenoceptor-independent mechanisms, demonstrating unknown properties for the agonists. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 12, 2009 Category: Drugs & Pharmacology Authors: Robert A. Ngala, Jacqueline O'Dowd, Steven J. Wang, Claire Stocker, Michael A. Cawthorne, Jonathan R.S. Arch Source Type: journals

β2-Adrenoceptor agonists alleviate neuropathic allodynia in mice after chronic treatmentEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Our data show that chronic treatment with [beta]-adrenoceptor agonists has the same antiallodynic properties as treatments with antidepressant drugs. This study was, however, conducted in an animal model, and a clinical validation will be required to confirm the value of the present findings in patients. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 12, 2009 Category: Drugs & Pharmacology Authors: Nada Choucair-Jaafar, Ipek Yalcin, Jean-Luc Rodeau, Elisabeth Waltisperger, Marie-José Freund-Mercier, Michel Barrot Source Type: journals

Effect of inhibition of extracellular signal-regulated kinase on relaxations to β-adrenoceptor agonists in porcine isolated blood vesselsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These data indicate that ERK inhibits [beta]2-adrenoceptor-mediated vasodilatation through a mechanism which may involve inactivation of plasma membrane potassium channels. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 11, 2009 Category: Drugs & Pharmacology Authors: CO Uhiara, SPH Alexander, RE Roberts Source Type: journals

The role of Epac proteins, novel cAMP mediators, in the regulation of immune, lung and neuronal functionEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Chronic degenerative inflammatory diseases, such as chronic obstructive pulmonary disease and Alzheimer's dementia, afflict millions of people around the world, causing death and debilitation. Despite the global impact of these diseases, there have been few innovative breakthroughs into their cause, treatment or cure. As with many debilitating disorders, chronic degenerative inflammatory diseases may be associated with defective or dysfunctional responses to second messengers, such as cyclic adenosinemonophosphate (cAMP). The identification of the cAMP-activated guanine nucleotide exchange factors for Ras-like GTPases, Epa...
Source: British Journal of Pharmacology - November 11, 2009 Category: Drugs & Pharmacology Authors: Maria Grandoch, Sara S. Roscioni, Martina Schmidt Source Type: journals

Endothelium modulates vasoconstrictor response to prostaglandin I2 in rat mesenteric resistance arteries: interaction between EP1 and TP receptorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: PGI2 activated the TP receptor in mesenteric resistance arteries and produced vasoconstriction, which the endothelium modulated through TP and EP1 receptors. PGI2 also released endothelium-derived hyperpolarizing factor and, through IP receptor activation, induced NO release, which in turn, was antagonized by TP and EP1 receptor activation. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 6, 2009 Category: Drugs & Pharmacology Authors: FE Xavier, J Blanco-Rivero, M Ferrer, G Balfagón Source Type: journals

Cyclic AMP-mediated chloride secretion is induced by prostaglandin F2α in human isolated colonEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: PGF2[alpha] stimulated chloride secretion in samples of human colon in vitro through a previously unrecognizd cAMP-mediated mechanism. These findings have implications for inflammatory states. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 5, 2009 Category: Drugs & Pharmacology Authors: D Collins, AM Hogan, MM Skelly, AW Baird, DC Winter Source Type: journals

3-Methylcholanthrene and benzo(a)pyrene modulate cardiac cytochrome P450 gene expression and arachidonic acid metabolism in male Sprague Dawley ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: 3-MC and BaP induce cardiac hypertrophy by increasing the ratio of DHETs : EETs and/or the ratio of 20-HETE : total EETs, through increasing soluble epoxide hydrolase activity. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 4, 2009 Category: Drugs & Pharmacology Authors: Mona E Aboutabl, Beshay NM Zordoky, Ayman OS El-Kadi Source Type: journals

Enhancement of the anti-inflammatory and anti-arthritic effects of theophylline by a low dose of a nitric oxide donor or non-specific nitric oxide synthase inhibitorEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and Implication: These findings confirm the anti-inflammatory and anti-arthritic activities of theophylline and suggest a new approach to enhance the anti-inflammatory and anti-arthritic effects of theophylline would be to administer it in combination with a low dose of a NO donor or a non-specific NO synthase inhibitor. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 4, 2009 Category: Drugs & Pharmacology Authors: Adel Gomaa, Mohsen Elshenawy, Noha Afifi, Eman Mohammed, Romany Thabit Source Type: journals

Trafficking and signalling of gonadotrophin-releasing hormone receptors: an automated imaging approachEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Gonadotrophin-releasing hormone (GnRH) is a neuropeptide that mediates central control of reproduction by stimulating gonadotrophin secretion from the pituitary. It acts via 7 transmembrane region (7TM) receptors that lack C-terminal tails, regions that for many 7TM receptors, are necessary for agonist-induced phosphorylation and arrestin binding as well as arrestin-dependent desensitization, internalization and signalling. Recent work has revealed that human GnRH receptors (GnRHR) are poorly expressed at the cell surface. This apparently reflects inefficient exit from the endoplasmic reticulum, which is thought to be incr...
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: AR Finch, KR Sedgley, SP Armstrong, CJ Caunt, CA McArdle Source Type: journals

Nitrite, NO and hypoxic vasodilationEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The ability to deliver oxygen and other nutrients to working tissues at a rate acutely matched to demand is the quintessential function of the cardiovascular system. Thus, an understanding of the biochemical mechanisms involved in hypoxic vasodilation remains a major goal in vascular biology. Nitric oxide, its metabolites, and oxidation status are recognized as playing important roles in this process. Previous work examining how nitrite can be converted to bioactive nitric oxide (NO) under hypoxic conditions has focused on the role of the red blood cell and haemoglobin. In a recent issue of the British Journal of Pharmacol...
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: Jason D Allen, Andrew J Gow Source Type: journals

α1A/B-Knockout mice explain the native α1D-adrenoceptor's role in vasoconstriction and show that its location is independent of the other α1-subtypesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: 'Pure'[alpha]1D-adrenoceptor pharmacology in [alpha]1A/B-KO provides a quantitative standard. Functionally, the [alpha]1D- and [alpha]1A-adrenoceptors produce additive responses and do not significantly compensate for each other. [alpha]1D-Adrenoceptor contributes to sensitivity even in resistance arteries. In [alpha]1A/B-KO, the loss of [alpha]1A- and [alpha]1B-adrenoceptors is reflected by a general decrease in fluorescence, but similar binding distribution to WT indicates that the [alpha]1D-adrenoceptor location in native smooth-muscle cells is not influenced by other [alpha]1-adrenoceptors...
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: L Methven, PC Simpson, JC McGrath Source Type: journals

Levetiracetam inhibits glutamate transmission through presynaptic P/Q-type calcium channels on the granule cells of the dentate gyrusEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These results suggest that levetiracetam modulated the presynaptic P/Q-type voltage-dependent calcium channel to reduce glutamate release and inhibited the amplitude of EPSC in DG. This effect is most likely to contribute to the anti-epileptic action of levetiracetam in patients. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: Chun-Yao Lee, Chih-Chuan Chen, Horng-Huei Liou Source Type: journals

Geranylgeraniol prevents the cytotoxic effects of mevastatin in THP-1 cells, without decreasing the beneficial effects on cholesterol synthesisEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Geranylgeraniol had a broader protective effect against the cytotoxicity of statins than exogenous ubiquinone. Therefore, geranylgeraniol may be a more useful and practical means of limiting the toxicities of statins, without reducing their efficacy as cholesterol lowering agents. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: I Campia, C Lussiana, G Pescarmona, D Ghigo, A Bosia, C Riganti Source Type: journals

β-arrestins – scaffolds and signalling elements essential for WNT/Frizzled signalling pathways?Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
[beta]-arrestins were originally identified as negative regulators of G protein-coupled receptor signalling. Recent studies have revealed that [beta]-arrestins serve as intracellular scaffolds and signalling intermediates. Their diverse functions in intracellular signalling pathways provide mechanisms for achieving signal specificity that might be attacked for pharmacological intervention. Here, we summarize the importance of [beta]-arrestin function for WNT [wingless (from Drosophila) and the oncogene int-1]/Frizzled (FZD) signalling. WNTs are secreted lipoglycoproteins that act through the seven transmembrane-spanning re...
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: Gunnar Schulte, Alexandra Schambony, Vítězslav Bryja Source Type: journals

Characterization of the oestrogenic activity of non-aromatic steroids: are there male-specific endogenous oestrogen receptor modulators?Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These results provide evidence for the possibility that some of the endogenous androgen precursors or metabolites could serve as male-specific ER ligands. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - November 3, 2009 Category: Drugs & Pharmacology Authors: Pan Wang, Yujing Wen, Gui-Zhen Han, Pritam Kaur Sidhu, Bao Ting Zhu Source Type: journals

Release of ATP from rat urinary bladder mucosa: role of acid, vanilloids and stretchEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Capsaicin (at TRPV1) and acid (at both TRPV1 and ASIC) induce ATP release from the rat bladder mucosa. This ATP appears to be principally of urothelial origin. This study highlights the importance of ATP and acid as signalling molecules in modulating bladder function. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 27, 2009 Category: Drugs & Pharmacology Authors: P Sadananda, F Shang, L Liu, KJ Mansfield, E Burcher Source Type: journals

Desensitization of endothelial P2Y1 receptors by PKC-dependent mechanisms in pressurized rat small mesenteric arteriesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These data demonstrate for the first time the involvement of PKC in the desensitization of endothelial P2Y1 receptors in pressurized rat mesenteric arteries, which may have important implications in the control of blood flow by circulating nucleotides. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 20, 2009 Category: Drugs & Pharmacology Authors: R Rodríguez-Rodríguez, P Yarova, P Winter, KA Dora Source Type: journals

NS11021, a novel opener of large-conductance Ca2+-activated K+ channels, enhances erectile responses in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: NS11021 leads to relaxation of both intracavernous arteries and corpus cavernosum strips primarily through opening of BKCa channels. It is also effective in facilitating erectile responses in anaesthetized rats. These results suggest a potential for use of BKCa openers in the treatment of ED. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: A Kun, VV Matchkov, E Stankevicius, A Nardi, AD Hughes, HJ Kirkeby, J Demnitz, U Simonsen Source Type: journals

Further pharmacological characterization of 5-HT2C receptor agonist-induced inhibition of 5-HT neuronal activity in the dorsal raphe nucleus in vivoEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These data strengthen the hypothesis that midbrain 5-HT neurones are under the inhibitory control of 5-HT2C receptors, and suggest that the 5-HT2C agonists Ro 60-0175, mCPP and WAY 161503, but not LSD or MDMA, are useful probes of the mechanism(s) involved. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: P Quérée, S Peters, T Sharp Source Type: journals

Beneficial effect of a hydrogen sulphide donor (sodium sulphide) in an ovine model of burn- and smoke-induced acute lung injuryEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Parenteral administration of the H2S donor ameliorated the pulmonary pathophysiological changes associated with burn- and smoke-induced acute lung injury. Based on the effect of H2S observed in this clinically relevant model of disease, we propose that treatment with H2S or its donors may represent a potential therapeutic strategy in managing patients with acute lung injury. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: Aimalohi Esechie, Perenlei Enkhbaatar, Daniel L Traber, Collette Jonkam, Matthias Lange, Atsumori Hamahata, Clarisse Djukom, Elbert B Whorton, Hal K Hawkins, Lillian D Traber, Csaba Szabo Source Type: journals

Inhibition of nitric oxide-activated guanylyl cyclase by calmodulin antagonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: The disruption of every stage of NO signal transduction by common CaM antagonists, unrelated to CaM antagonism, cautions against their utility as pharmacological tools. More positively, the compounds exemplify a novel class of sGC inhibitors that, with improved selectivity, may be therapeutically valuable. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: LR James, CH Griffiths, J Garthwaite, TC Bellamy Source Type: journals

Haem oxygenase-1 induction protects against tumour necrosis factor α impairment of endothelial-dependent relaxation in rat isolated pulmonary arteryEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Induction of HO-1 protected against TNF[alpha] impairment of endothelium-dependent relaxation in pulmonary artery, by a mechanism involving a reduction in inducible NO synthase-derived NO production. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: Hany M. El-Bassossy, Nabila N. El-Maraghy, Hassan M. El-Fayoumi, Malcolm L. Watson Source Type: journals

Effect of tecarfarin, a novel vitamin K epoxide reductase inhibitor, on coagulation in beagle dogsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: Overall, the data presented herein indicate that tecarfarin, via a vitamin K-dependent mechanism, causes changes in key parameters of haemostasis in beagle dogs that are consistent with effective anticoagulation. Compared to warfarin it has a decreased potential to interact metabolically with drugs that inhibit CYP450 enzymes and, therefore, may offer an improved safety profile for patients. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: A Choppin, I Irwin, L Lach, MG McDonald, AE Rettie, L Shao, C Becker, MP Palme, X Paliard, S Bowersox, DM Dennis, P Druzgala Source Type: journals

Hyperlipidaemia induced by a high-cholesterol diet leads to the deterioration of guanosine-3',5'-cyclic monophosphate/protein kinase G-dependent cardioprotection in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: This is the first demonstration that defects in the cardioprotective cGMP[ndash]PKG system could be a critical biochemical anomaly in hyperlipidaemia. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: Z Giricz, A Görbe, J Pipis, DS Burley, P Ferdinandy, GF Baxter Source Type: journals

Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Background and purpose: Several agonists of the [alpha]7 nicotinic acetylcholine receptor (nAChR) have been developed for treatment of cognitive deficits. However, agonist efficacy in vivo is difficult to reconcile with rapid [alpha]7 nAChR desensitization in vitro; and furthermore, the correlation between in vitro receptor efficacy and in vivo behavioural efficacy is not well delineated. The possibility that agonists of this receptor actually function in vivo as inhibitors via desensitization has not been finally resolved.Experimental approach: Two structurally related [alpha]7 nAChR agonists were characterized and used t...
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: Clark A Briggs, Jens Halvard Grønlien, Peter Curzon, Daniel B Timmermann, Hilde Ween, Kirsten Thorin-Hagene, Paige Kerr, David J Anderson, John Malysz, Tino Dyhring, Gunnar M Olsen, Dan Peters, William H Bunnelle, Murali Gopalakrishnan Source Type: journals

Effect of the CB1 receptor antagonists rimonabant and AM251 on the firing rate of dorsal raphe nucleus neurons in rat brain slicesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: These results suggest a tonic/constitutive regulation of DRN 5-HT neurons by the endocannabinoid system, which may occur through a CB1 receptor-mediated inhibition of the GABAergic system. The inhibitory effect of anandamide may be mediated through a CB1 receptor-independent mechanism. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: Aitziber Mendiguren, Joseba Pineda Source Type: journals

Effects of 7,8-dihydro-8-oxo-deoxyguanosine on antigen challenge in ovalbumin-sensitized mice may be mediated by suppression of RacEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion and implications: 8-Oxo-dG had anti-allergic actions that might be mediated by Rac inactivation. This compound merits further evaluation of its therapeutic potential in allergic asthma. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: JY Ro, DY Kim, S-H Lee, JW Park, M-H Chung Source Type: journals

Subtype-selective targeting of voltage-gated sodium channelsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Voltage-gated sodium channels are key to the initiation and propagation of action potentials in electrically excitable cells. Molecular characterization has shown there to be nine functional members of the family, with a high degree of sequence homology between the channels. This homology translates into similar biophysical and pharmacological properties. Confidence in some of the channels as drug targets has been boosted by the discovery of human mutations in the genes encoding a number of them, which give rise to clinical conditions commensurate with the changes predicted from the altered channel biophysics. As a result,...
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: Steve England, Marcel J de Groot Source Type: journals

Transient receptor potential ankyrin receptor 1 is a novel target for pro-tussive agentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions and implications: A novel pro-tussive pathway involves the TRPA1 channel, expressed by capsaicin-sensitive airway sensory nerves and is activated by a series of exogenous (cigarette smoke) and endogenous irritants. These results suggest TRPA1 may be a novel target for anti-tussive medicines. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 19, 2009 Category: Drugs & Pharmacology Authors: E Andrè, R Gatti, M Trevisani, D Preti, PG Baraldi, R Patacchini, P Geppetti Source Type: journals