Characterization of Gaddum's substance R.

abstract：BACKGROUND AND PURPOSE:Recent studies suggest that the effects of cyclooxygenase-2 (COX-2) inhibition are mediated by cannabinoid receptor activation. However, some non-steroidal anti-inflammatory drugs inhibit the enzyme fatty acid amide hydrolase, which regulates levels of some endocannabinoids. Whether COX-2 directl...

journal_title：British journal of pharmacology

authors： Staniaszek LE,Norris LM,Kendall DA,Barrett DA,Chapman V

更新日期：2010-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Diabetes is a risk factor for the development of coronary artery disease but it is not known whether the functions of endothelium-derived nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) in coronary arteries are altered in the early stage of diabetes. Such alterations and t...

journal_title：British journal of pharmacology

authors： Kajikuri J,Watanabe Y,Ito Y,Ito R,Yamamoto T,Itoh T

更新日期：2009-09-01 00:00:00

abstract：:AMPA-type glutamate receptors are one of the most dynamic components of excitatory synapses. Their regulated addition and removal from synapses leads to long-lasting forms of synaptic plasticity, known as long-term potentiation (LTP) and long-term depression (LTD). In addition, AMPA receptors reach their synaptic targ...

journal_title：British journal of pharmacology

authors： Esteban JA

更新日期：2008-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Selective cannabinoid CB2 receptor agonists have demonstrated analgesic activity across multiple preclinical pain models. AM1241 is an indole derivative that exhibits high affinity and selectivity for the CB2 binding site and broad spectrum analgesic activity in rodent models, but is not an antag...

journal_title：British journal of pharmacology

authors： Yao BB,Hsieh GC,Frost JM,Fan Y,Garrison TR,Daza AV,Grayson GK,Zhu CZ,Pai M,Chandran P,Salyers AK,Wensink EJ,Honore P,Sullivan JP,Dart MJ,Meyer MD

更新日期：2008-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pharmacokinetic/pharmacodynamic (PK/PD) models are necessary to relate the degree of drug exposure in vivo to target blockade and pharmacological efficacy. This manuscript describes a murine agonist-induced CXCR3 receptor internalization assay and demonstrates its utility for PK/PD analyses. EXP...

journal_title：British journal of pharmacology

authors： Jopling LA,Watt GF,Fisher S,Birch H,Coggon S,Christie MI

更新日期：2007-12-01 00:00:00

abstract：:GPCRs can interact with each other to form homomers or heteromers. Homomers involve interactions with the same receptor type while heteromers involve interactions between two different GPCRs. These receptor-receptor interactions modulate not only the binding but also the signalling and trafficking properties of indivi...

journal_title：British journal of pharmacology

authors： Fujita W,Gomes I,Devi LA

更新日期：2014-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The human, rat, and mouse P2X(7) receptors have been previously characterized, and in this study we report the cloning and pharmacological properties of the guinea pig orthologue. EXPERIMENTAL APPROACH:A cDNA encoding for the guinea pig P2X(7) receptor was isolated from a guinea pig brain librar...

journal_title：British journal of pharmacology

authors： Fonfria E,Clay WC,Levy DS,Goodwin JA,Roman S,Smith GD,Condreay JP,Michel AD

更新日期：2008-02-01 00:00:00

abstract：:1. The effects of dopamine on the L-type Ca2+ current (ICa,L) of both atrial and ventricular single myocytes and on the force of contraction of atrial trabeculae in rat heart were investigated. 2. Dopamine increased atrial ICa,L at concentrations higher than 1 microM, but had little or no effect on ICa,L at lower conc...

journal_title：British journal of pharmacology

authors： Zhao H,Matsuoka S,Fujioka Y,Noma A

更新日期：1997-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Dexmedetomidine, an alpha(2)-adrenoceptor agonist, exhibits anti-nociceptive actions at the spinal cord and enhances the effect of local anaesthetics in the peripheral nervous system. Although the latter action may be attributed in part to inhibition of nerve conduction produced by dexmedetomidin...

journal_title：British journal of pharmacology

authors： Kosugi T,Mizuta K,Fujita T,Nakashima M,Kumamoto E

更新日期：2010-08-01 00:00:00

abstract：:1 The effects of isoprenaline, propranolol and phosphodiesterase inhibitors on (3)H-transmitter overflow elicited by low frequency nerve stimulation were determined in the isolated perfused spleen of the cat.2 (-)-Isoprenaline (0.14, 1.4, and 14 nM) produced a concentration-dependent increase in [(3)H]-transmitter ove...

journal_title：British journal of pharmacology

authors： Celuch SM,Dubocovich ML,Lander SZ

更新日期：1978-05-01 00:00:00

abstract：:1. In the present study we tested the hypothesis that insulin-like growth factor-1 (IGF-1) modulates resting chloride conductance (G(Cl)) of rat skeletal muscle by activating a phosphatase and that the chloride channel, based on the activity of phosphorylating-dephosphorylating pathways, has different sensitivity to s...

journal_title：British journal of pharmacology

authors： De Luca A,Pierno S,Liantonio A,Camerino C,Conte Camerino D

更新日期：1998-10-01 00:00:00

abstract：:1. The interactions between two K+ channel openers, cromakalim and SR 44866 (infused i.v. at equihypotensive doses), and the sympathetic nervous system at the systemic and regional (mesentery, kidney, hindlimb) vascular levels were investigated in the pithed spontaneously hypertensive rat (SHR) by use of the pulsed Do...

journal_title：British journal of pharmacology

authors： Richer C,Mulder P,Doussau MP,Gautier P,Giudicelli JF

更新日期：1990-07-01 00:00:00

abstract：:Three genes encode the small-conductance Ca(2+)-activated K(+) channels (SK channels). We have stably expressed hSK1 and rSK2 in HEK 293 cells and addressed the pharmacology of these subtypes using whole-cell patch clamp recordings. The bee venom peptide apamin blocked hSK1 as well as rSK2 with IC(50) values of 3.3 nM...

journal_title：British journal of pharmacology

authors： Strøbaek D,Jørgensen TD,Christophersen P,Ahring PK,Olesen SP

更新日期：2000-03-01 00:00:00

abstract：:Almost all existing models for G-protein-coupled receptors (GPCRs) are based on the occurrence of monomers. Recent studies show that many GPCRs are dimers. Therefore for some receptors dimers and not monomers are the main species interacting with hormones/neurotransmitters/drugs. There are reasons for equivocal interp...

journal_title：British journal of pharmacology

authors： Franco R,Casadó V,Cortés A,Mallol J,Ciruela F,Ferré S,Lluis C,Canela EI

更新日期：2008-03-01 00:00:00

abstract：:Liver X receptors (LXRs) are members of the nuclear receptor superfamily that are canonically activated by oxidized derivatives of cholesterol. Since the mid-90s, numerous groups have identified LXRs as endocrine receptors that are involved in the regulation of various physiological functions. As a result, when their ...

journal_title：British journal of pharmacology

authors： Buñay J,Fouache A,Trousson A,de Joussineau C,Bouchareb E,Zhu Z,Kocer A,Morel L,Baron S,Lobaccaro JA

更新日期：2020-10-20 00:00:00

abstract：:1. In the presence of indomethacin (IM, 10 microM) and N omega-nitro-L- arginine (L-NOARG, 0.3 mM), acetylcholine (ACh) induces an endothelium-dependent smooth muscle hyperpolarization and relaxation in the rat isolated hepatic artery. The potassium (K) channel inhibitors, tetrabutylammonium (TBA, 1 mM) and to a lesse...

journal_title：British journal of pharmacology

authors： Zygmunt PM,Högestätt ED

更新日期：1996-04-01 00:00:00

abstract：:Interleukin-2 (IL-2), an immunoregulatory cytokine possessing antitumour activity, is an inducer of nitric oxide (NO) synthesis in mice and man. In this study, the possibility that IL-2 possesses antiangiogenic properties that account for its antitumour effects in vivo was examined. IL-2 caused a dose-dependent inhibi...

journal_title：British journal of pharmacology

authors： Sakkoula E,Pipili-Synetos E,Maragoudakis ME

更新日期：1997-11-01 00:00:00

abstract：:1. The effect of in vivo desensitization to leukotriene B4 (LTB4) on eosinophil infiltration in response to recombinant C5a was examined in guinea-pig skin. 2. LTB4 (10-300 ng) and C5a (1-10 micrograms) caused a dose-dependent increase in the levels of eosinophil peroxidase activity (a measure of eosinophil infiltrati...

journal_title：British journal of pharmacology

authors： Pettipher ER,Salter ED,Showell HJ

更新日期：1994-09-01 00:00:00

abstract：:1. The present study was designed to investigate tolerance to several pharmacological effects of apomorphine. 2. Changes in blood pressure, heart rate, plasma noradrenaline levels, rectal temperature, respiratory rate and retching plus vomiting were compared after administration of apomorphine (200 micrograms kg-1, i....

journal_title：British journal of pharmacology

authors： Montastruc JL,Llau ME,Senard JM,Tran MA,Rascol O,Montastruc P

更新日期：1996-03-01 00:00:00

abstract：:1 The binding of [3H]-5-hydroxytryptamine ([3H]-5-HT), [3H]-haloperidol and [3H]-dopamine to human blood platelets was investigated and the effects of unlabelled haloperidol on [3H]-5-HT binding and (+)- and (-)-butaclamol on [3H]-haloperidol were studied. 2 Scatchard analysis did not show any specific binding of [3H]...

journal_title：British journal of pharmacology

authors： Boullin DJ,Molyneux D,Roach B

更新日期：1978-07-01 00:00:00

abstract：:1 Burimamide injected intravenously in the anaesthetized or conscious cat produced significant increases in gastric acid secretion: in the anaesthetized cat it produced increased gastric mucosal blood flow. 2 Metiamide, in doses which inhibited pentagastrin-stimulated acid secretion, produced no increase in gastric ac...

journal_title：British journal of pharmacology

authors： Harris DW,Smy JR,Reed JD,Venables CW

更新日期：1975-02-01 00:00:00

abstract：:1. The NK1 tachykinin receptor agonists, septide, [Sar9,Met(O2)11]SP and [Pro9]SP produced locomotor hyperactivity (10-20 min) when injected intracerebroventricularly (i.c.v.) in the guinea-pig. The most potent in eliciting this hyperactivity was septide (from 0.63 to 5 micrograms), compared to [Sar9,Met(O2)11]SP, whi...

journal_title：British journal of pharmacology

authors： Piot O,Betschart J,Grall I,Ravard S,Garret C,Blanchard JC

更新日期：1995-11-01 00:00:00

abstract：:1. The cyclic nucleotide phosphodiesterase (PDE) of guinea-pig eosinophils was partially characterized and the effects of selective inhibitors of PDE isoenzymes upon opsonized zymosan (OZ)-stimulated respiratory burst were studied. 2. PDE activity in eosinophil lysates appeared to be membrane-associated, displayed sub...

journal_title：British journal of pharmacology

authors： Dent G,Giembycz MA,Rabe KF,Barnes PJ

更新日期：1991-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Down's syndrome is a common genetic cause of intellectual disability, for which there are no drug therapies. Mechanistic studies in a model of Down's syndrome [Ts65Dn (TS) mice] demonstrated that impaired cognitive function was due to excessive neuronal inhibitory tone. These deficits were normal...

journal_title：British journal of pharmacology

authors： Colas D,Chuluun B,Warrier D,Blank M,Wetmore DZ,Buckmaster P,Garner CC,Heller HC

更新日期：2013-07-01 00:00:00

abstract：:1. The potencies of some beta-adrenoreceptor blocking drugs in reducing noradrenaline uptake by the isolated heart were compared with their potencies in reducing the release of noradrenaline from the heart by tyramine.2. Of the drugs tested, propranolol, pronethalol and dichloroisoprenaline were the most potent in blo...

journal_title：British journal of pharmacology

authors： Foo JW,Jowett A,Stafford A

更新日期：1968-09-01 00:00:00

abstract：:Histamine has been one of the most studied substances in medicine, playing a major role in diverse (patho)physiological processes. It elicits its multifaceted modulatory functions by activating four types of GPCRs, designated as H1-4 . Despite the heterogeneity and the complexity of histamine receptor pharmacology, ma...

journal_title：British journal of pharmacology

authors： Tiligada E,Ennis M

更新日期：2020-02-01 00:00:00

abstract：:1. Piperazinylindoles (DPI 201-106, BDF 8784), drugs known to act on voltage-dependent Na(+)-channels, bind with very high affinity to a Ca2(+)-channel-associated phenylalkylamine receptor in Drosophila melanogaster head membranes. These compounds and (+)-tetrandrine, a naturally occurring Ca2(+)-antagonist, were the ...

journal_title：British journal of pharmacology

authors： Glossmann H,Zech C,Striessnig J,Staudinger R,Hall L,Greenberg R,Armah BI

更新日期：1991-02-01 00:00:00

abstract：:The effects of carboxy-PTIO and hydroxocobalamin were studied on nitrergic transmission in anococcygeus and retractor penis muscles taken during post mortem examination from young male pigs. In both muscles under resting conditions, electrical field stimulation (EFS) caused contractions that were sensitive to tetrodot...

journal_title：British journal of pharmacology

authors： Li CG,Rand MJ

更新日期：1999-05-01 00:00:00

abstract：:1. Changes in cutaneous water loss were followed by continuously monitoring total body weight loss.2. Sweating was induced in normal subjects by raising the environmental temperature or by subjecting them to the emotional stress of mental arithmetic.3. Propranolol in a dosage of 0.15 mg/kg body weight intravenously ha...

journal_title：British journal of pharmacology

authors： Allen JA,Jenkinson DJ,Roddie IC

更新日期：1973-03-01 00:00:00

abstract：:1. The effects of the nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME) on vasoconstrictor responses to transmural electrical nerve stimulation and noradrenaline were examined in the rabbit isolated renal artery with and without an intact endothelium. In addition, the effect of removing the end...

journal_title：British journal of pharmacology

authors： Vials AJ,Crowe R,Burnstock G

更新日期：1997-05-01 00:00:00