The role of beta1- and beta2-adrenoceptors in the inhibition of gastric acid secretion in the dog.

abstract：:1. The effects of the selective alpha 2-adrenoceptor agonist, medetomidine, were assessed on plasma levels of immunoreactive atrial natriuretic peptide (IR-ANP), haemodynamics and on urine water and solute excretion in conscious, chronically cannulated, 7 month-old spontaneously hypertensive (SHR) and age-matched Wist...

journal_title：British journal of pharmacology

authors： Ruskoaho H,Leppäluoto J

更新日期：1989-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Suramin is a clinically prescribed drug for treatment of human African trypanosomiasis, cancer and infection. It is also a well-known pharmacological antagonist of P2 purinoceptors. Despite its clinical use and use in research, the biological actions of this molecule are still incompletely unders...

journal_title：British journal of pharmacology

authors： Chi Y,Gao K,Zhang H,Takeda M,Yao J

更新日期：2014-07-01 00:00:00

abstract：:1. In the neuronally isolated cortex of the cat, local application of bemegride, picrotoxin, nikethamide, caffeine and strychnine facilitated the surface positive response of the isolated cortex and lowered the stimulus threshold for this response. Excepting nikethamide, they all produced convulsive discharge in the i...

journal_title：British journal of pharmacology

authors： Frank GB,Jhamandas K

更新日期：1970-08-01 00:00:00

abstract：:Until recently, hydrogen sulfide (H2 S) was exclusively viewed a toxic gas and an environmental hazard, with its toxicity primarily attributed to the inhibition of mitochondrial Complex IV, resulting in a shutdown of mitochondrial electron transport and cellular ATP generation. Work over the last decade established mu...

journal_title：British journal of pharmacology

authors： Szabo C,Ransy C,Módis K,Andriamihaja M,Murghes B,Coletta C,Olah G,Yanagi K,Bouillaud F

更新日期：2014-04-01 00:00:00

abstract：:1. The present study was undertaken to investigate the effect of Delta9-tetrahydrocannabinol (Delta9-THC) and possible serotoninergic involvement on the extracellular level of dopamine (DA) in the striatum using microdialysis in conscious, freely-moving rats. 2. A dose-dependent increase in striatal DA release occurre...

journal_title：British journal of pharmacology

authors： Malone DT,Taylor DA

更新日期：1999-09-01 00:00:00

abstract：:The novel urotensin-II (U-II) receptor (UT) ligand, [Pen(5),DTrp(7),Dab(8)]U-II(4-11) (UFP-803), was pharmacologically evaluated and compared with urantide in in vitro and in vivo assays. In the rat isolated aorta, UFP-803 was inactive alone but, concentration dependently, displaced the contractile response to U-II to...

journal_title：British journal of pharmacology

authors： Camarda V,Spagnol M,Song W,Vergura R,Roth AL,Thompson JP,Rowbotham DJ,Guerrini R,Marzola E,Salvadori S,Cavanni P,Regoli D,Douglas SA,Lambert DG,Calò G

更新日期：2006-01-01 00:00:00

abstract：:Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonar...

journal_title：British journal of pharmacology

authors： Marsango S,Barki N,Jenkins L,Tobin AB,Milligan G

更新日期：2020-09-01 00:00:00

abstract：:1. The effect of 4-aminopyridine (4-AP) on the slow afterhyperpolarization (sAHP) seen after high frequency dendritic or somatic firing was investigated in rat hippocampal CA1 pyramidal neurones (PC). Intracellular recordings were obtained from the distal apical dendrites and somata and suprathreshold depolarizing cur...

journal_title：British journal of pharmacology

authors： Andreasen M

更新日期：2002-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Adrenoceptors can associate with cardiac caveolae. To investigate the function of vascular caveolae, adrenoceptor-mediated effects were compared in the saphenous artery of caveolin-1 knockout (cav-1KO) and wild-type (WT) mice. EXPERIMENTAL APPROACH:Electronmicroscopy was used to detect caveolae....

journal_title：British journal of pharmacology

authors： Neidhold S,Eichhorn B,Kasper M,Ravens U,Kaumann AJ

更新日期：2007-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Parabens are commonly added in pharmaceutical, cosmetic and food products because of their wide antibacterial properties, low toxicity, inertness and chemical stability, although the molecular mechanism of their antibacterial effect is not fully understood. Some agonists of the transient receptor...

journal_title：British journal of pharmacology

authors： Fujita F,Moriyama T,Higashi T,Shima A,Tominaga M

更新日期：2007-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary arterial hypertension (PAH) is characterized by enhanced pulmonary vascular resistance, right ventricular hypertrophy and increased right ventricular systolic pressure. Here, we investigated the effects of a N-acylhydrazone derivative, 3,4-dimethoxyphenyl-N-methyl-benzoylhydrazide (LASS...

journal_title：British journal of pharmacology

authors： Alencar AK,Pereira SL,Montagnoli TL,Maia RC,Kümmerle AE,Landgraf SS,Caruso-Neves C,Ferraz EB,Tesch R,Nascimento JH,de Sant'Anna CM,Fraga CA,Barreiro EJ,Sudo RT,Zapata-Sudo G

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Adenosine is considered to be an important modulator of intestinal motility. This study was undertaken to investigate the role of adenosine in the modulation of contractility in the mouse duodenum and to characterize the adenosine receptor subtypes involved. EXPERIMENTAL APPROACH:RT-PCR was used...

journal_title：British journal of pharmacology

authors： Zizzo MG,Mastropaolo M,Lentini L,Mulè F,Serio R

更新日期：2011-11-01 00:00:00

abstract：:In this issue of the British Journal of Pharmacology, Ryberg et al. present convincing in vitro evidence that the orphan GPCR, GPR55, is a cannabinoid receptor. GPR55 was activated by a range of plant, synthetic and endogenous cannabinoids and blocked by the non-psychoactive phytocannabinoid, cannabidiol. Their experi...

journal_title：British journal of pharmacology

authors： Pertwee RG

更新日期：2007-12-01 00:00:00

abstract：:1. Histamine and carbachol produced concentration-related increases in the accumulation of 3H-inositol phosphates in slices of bovine tracheal smooth muscle. 2. Noradrenaline alone produced a small stimulation of 3H-inositol phosphate accumulation which was inhibited by the alpha-adrenoceptor antagonist phentolamine. ...

journal_title：British journal of pharmacology

authors： Hall IP,Hill SJ

更新日期：1988-12-01 00:00:00

abstract：:1 The effect of potassium channel opening compounds has been investigated in the smooth muscle of rabbit aorta under Ca-free conditions. Examination of the characteristics of the response has been performed using cromakalim as the prototype compound. 2 In order of potency, Ro 31-6930, cromakalim, minoxidil sulphate an...

journal_title：British journal of pharmacology

authors： Duty S,Weston AH

更新日期：1992-12-01 00:00:00

abstract：:1. The effects of sodium nitroprusside (SNP, a nitric oxide donor) and authentic nitric oxide (NO) on superoxide anion (O2-) generation were investigated in human polymorphonuclear leukocytes (PMNs). 2. Neither SNP (10 nM to 10 microM) nor NO (40 nM to 40 microM) alone induced O2- generation or change of intracellular...

journal_title：British journal of pharmacology

authors： Morikawa M,Inoue M,Tokumaru S,Kogo H

更新日期：1995-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:alpha5IA (3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine) is a triazolophthalazine with subnanomolar affinity for alpha1-, alpha2-, alpha3- and alpha5-containing GABA(A) receptors. Here we have evaluated the relationship between plasma alpha5...

journal_title：British journal of pharmacology

authors： Atack JR,Eng WS,Gibson RE,Ryan C,Francis B,Sohal B,Dawson GR,Hargreaves RJ,Burns HD

更新日期：2009-07-01 00:00:00

abstract：:Two-state and operational models of both agonism and allosterism are compared to identify and characterize common pharmacological parameters. To account for the receptor-dependent basal response, constitutive receptor activity is considered in the operational models. By arranging two-state models as the fraction of ac...

journal_title：British journal of pharmacology

authors： Roche D,Gil D,Giraldo J

更新日期：2013-07-01 00:00:00

abstract：:1. Peroxynitrite, a potent cytotoxic oxidant formed by the reaction of nitric oxide with superoxide anion, and hydroxyl radical, formed in the iron-catalysed Fenton reaction, are important mediators of reperfusion injury. In in vitro studies, DNA single strand breakage, triggered by peroxynitrite or by hydroxyl radica...

journal_title：British journal of pharmacology

authors： Cuzzocrea S,Zingarelli B,Costantino G,Szabó A,Salzman AL,Caputi AP,Szabó C

更新日期：1997-07-01 00:00:00

abstract：:1. In order to define the electrophysiological mechanism(s) responsible for bradykinin (BK)-induced positive inotropic and chronotropic responses in isolated guinea-pig atria, effects of BK on the membrane currents were examined in isolated atrial cells using patch clamp techniques. 2. BK (0.1-1000 nM) increased the L...

journal_title：British journal of pharmacology

authors： Sakamoto N,Uemura H,Hara Y,Saito T,Masuda Y,Nakaya H

更新日期：1998-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Injury to the lung parenchyma is a constitutional feature shared by many lung diseases. The protein, phosphatase and tensin homologue deleted on chromosome Ten (PTEN) is a major suppressor of phosphoinositide-3 kinase/Akt signalling, a vital survival pathway in lung parenchymal cells. Based on th...

journal_title：British journal of pharmacology

authors： Lai JP,Bao S,Davis IC,Knoell DL

更新日期：2009-01-01 00:00:00

abstract：:An investigation of the effects of gamma-aminobutyric acid (GABA) and the selective GABAB receptor agonist, baclofen, on basal and stimulated adenosine 3':5'-cyclic monophosphate (cyclic AMP) levels in slices of rat cerebral cortex has been carried out. Neither GABA nor baclofen produced any significant change in basa...

journal_title：British journal of pharmacology

authors： Hill DR

更新日期：1985-01-01 00:00:00

abstract：:1. Noradrenaline 1 microM induced a contractile response in rat isolated aorta in the presence or in the absence of extracellular Ca2+ with depletion of intracellular Ca2+ stores. Thereafter, during incubation in the presence of Ca2+, an increase in the resting tone was observed. Such a contractile response did not oc...

journal_title：British journal of pharmacology

authors： Noguera MA,D'Ocon MP

更新日期：1993-10-01 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 activity pattern of analogues of the enkephalins was determined in four parallel assays, the inhibition of the electrically evoked contraction of the guinea-pig ileum and mouse vas deferens at 36 degrees C and the inhibition of [(3)H]-naltrexone and [(3)H]-leucine-enkephalin binding at 0 to 4 degrees C in homoge...

journal_title：British journal of pharmacology

authors： Kosterlitz HW,Lord JA,Paterson SJ,Waterfield AA

更新日期：1980-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibitory neurotransmission plays an important role in controlling excitability within nociceptive circuits of the spinal cord dorsal horn. Loss of inhibitory signalling is thought to contribute to the development of pathological pain. Preclinical studies suggest that increasing inhibitory glyci...

journal_title：British journal of pharmacology

authors： Winters BL,Rawling T,Vandenberg RJ,Christie MJ,Bhola RF,Imlach WL

更新日期：2018-06-01 00:00:00

abstract：:1. We investigated the role of two conserved basic residues in the second transmembrane helix arginine 172 (R172) and lysine 179 (K179) of the VPAC(2) receptor. 2. Vasoactive intestinal polypeptide (VIP) activated VPAC(2) receptors with an EC(50) value of 7 nM, as compared to 150, 190 and 4000 nM at R172L, R172Q and K...

journal_title：British journal of pharmacology

authors： Vertongen P,Solano RM,Perret J,Langer I,Robberecht P,Waelbroeck M

更新日期：2001-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The effects of 4-O-methylhonokiol (MH), a constituent of Magnolia officinalis, were investigated on human prostate cancer cells and its mechanism of action elucidated. EXPERIMENTAL APPROACH:The anti-cancer effects of MH were examined in prostate cancer and normal cells. The effects were validate...

journal_title：British journal of pharmacology

authors： Lee NJ,Oh JH,Ban JO,Shim JH,Lee HP,Jung JK,Ahn BW,Yoon DY,Han SB,Ham YW,Hong JT

更新日期：2013-03-01 00:00:00

abstract：:Alcohol-use disorders are chronically relapsing conditions characterized by cycles of use, abstinence and relapse. The ventral pallidum (VP) is a key node in the neural circuits controlling relapse to alcohol seeking and a key target of pharmacotherapies for relapse prevention. There has been a significant increase in...

journal_title：British journal of pharmacology

authors： Prasad AA,McNally GP

更新日期：2020-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Small molecule glucokinase activators (GKAs) have been associated with potent antidiabetic efficacy and hepatic steatosis in rodents. This study reports the discovery of S 50131 and S 51434, two novel GKAs with an original scaffold and an atypical pharmacological profile. EXPERIMENTAL APPROACH:A...

journal_title：British journal of pharmacology

authors： De Ceuninck F,Kargar C,Charton Y,Goldstein S,Perron-Sierra F,Ilic C,Caliez A,Rolin JO,Sadlo M,Harley E,Vinson C,Ktorza A

更新日期：2013-07-01 00:00:00