Electrophysiological study of SR 42641, a novel aminopyridazine derivative of GABA: antagonist properties and receptor selectivity of GABAA versus GABAB responses.

abstract：:1. The current study investigated the effects of respiratory tract viral infection on the density of ETA and ETB receptors in murine tracheal smooth muscle and on the contractile response to endothelin-1 mediated by these receptors. 2. Quantitative autoradiographic studies using [125I]-endothelin-1 revealed that trach...

journal_title：British journal of pharmacology

authors： Henry PJ,Goldie RG

更新日期：1994-08-01 00:00:00

abstract：:1. [3H]-ouabain uptake in resting guinea-pig papillary muscles depended directly on incubation time and inversely with muscle radius. The equivalence of both parameters support the relevance of diffusion. A particular mechanism of receptor-controlled diffusion was implicated by the saturation of initial rates of uptak...

journal_title：British journal of pharmacology

authors： Ebner F,Siegl H

更新日期：1988-10-01 00:00:00

abstract：:1 The N6-2-O-dibutyryl derivative of adenosine 3',5'-monophosphate (db cyclic AMP) has been micro-injected into the third cerebral ventricle of the unanaesthetized, restrained mouse and the effects on body temperature and thermoregulatory activities observed. 2 Db cyclic AMP (4, 16 and 32 micrograms) injected intracer...

journal_title：British journal of pharmacology

authors： Dascombe MJ,Milton AS,Nyemitei-Addo I,Pertwee RG

更新日期：1980-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Leucocyte infiltration is a rate-limiting step in the pathophysiology of acute pancreatitis (AP) although the adhesive mechanisms supporting leucocyte-endothelium interactions in the pancreas remain elusive. The aim of this study was to define the role of lymphocyte function antigen-1 (LFA-1) in ...

journal_title：British journal of pharmacology

authors： Awla D,Abdulla A,Zhang S,Roller J,Menger MD,Regnér S,Thorlacius H

更新日期：2011-05-01 00:00:00

abstract：:Photorelaxation of vascular smooth muscle (VSM) is caused by the release of nitric oxide (NO) from a finite molecular store that can be depleted by irradiating pre-contracted arteries with visible light. The ability of an 'exhausted' vessel to respond to a further period of illumination is lost temporarily but then re...

journal_title：British journal of pharmacology

authors： Megson IL,Holmes SA,Magid KS,Pritchard RJ,Flitney FW

更新日期：2000-08-01 00:00:00

abstract：:1. The rat spinal cord in vitro has been used to assess the effect of 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) on the dorsal root evoked extracellular ventral root reflex (DR-VRR) and the intracellular excitatory postsynaptic potential (e.p.s.p.) in ventral horn neurones and motoneurones. 2. CNQX (1-5 microM) produ...

journal_title：British journal of pharmacology

authors： King AE,Lopez-Garcia JA,Cumberbatch M

更新日期：1992-10-01 00:00:00

abstract：:1. We investigated the cytoprotective effect of low-dose nitric oxide (NO) on NO-induced cell death in mouse macrophage-like cell line RAW264. 2. Sodium nitroprusside (SNP), an NO donor, at a high concentration (4 mM) released cytochrome c from mitochondria and induced death in RAW264 cells. Acetyl-L-aspartyl-L-glutam...

journal_title：British journal of pharmacology

authors： Yoshioka Y,Yamamuro A,Maeda S

更新日期：2003-05-01 00:00:00

abstract：:The effect of the selective serotonin reuptake inhibitor fluoxetine was examined on the 5-HT4 receptor-mediated relaxation in the rat isolated ileum. Fluoxetine unsurmountably antagonized the relaxation to exogenous 5-HT with abolition of the response at 10 microM. Fluoxetine (10 microM) also caused a gradual loss of ...

journal_title：British journal of pharmacology

authors： Tuladhar BR,Costall B,Naylor RJ

更新日期：2002-05-01 00:00:00

abstract：:The effects of treatment with rolipram, a specific phosphodiesterase IV inhibitor, on learning and memory function and on the cyclic AMP/PKA/CREB signal transduction system were examined in rats with microsphere embolism (ME)-induced cerebral ischaemia. Sustained cerebral ischaemia was induced by the injection of 900 ...

journal_title：British journal of pharmacology

authors： Nagakura A,Niimura M,Takeo S

更新日期：2002-04-01 00:00:00

abstract：:1. The 37 amino acid human calcitonin gene-related peptide (CGRP), was injected intra-arterially into the isolated, blood perfused spleen of the dog. 2. The only vascular response observed to CGRP, once threshold had been reached (10-20 fmol), was a dose-dependent splenic arterial vasodilatation. 3. The mean intra-art...

journal_title：British journal of pharmacology

authors： Withrington PG

更新日期：1989-04-01 00:00:00

abstract：:1. The purpose of this study was to determine the in vivo inhibitory efficacy of azapropazone on neutrophil migration. The effects of azapropazone given at a dose of 100 mg kg-1 i.v. every 2 h on the neutrophil migration into skin inflammation sites (blister fluid) as well as into an autologous serum (+/- chemoattract...

journal_title：British journal of pharmacology

authors： Mousa SA,Brown R,Chan Y,Hsieh J,Smith RD

更新日期：1990-02-01 00:00:00

abstract：:1. Mouse islets were used to define the characteristics and study the mechanisms of the stimulation of insulin release by compound AZ-DF 265, 4-[[N-(alpha-phenyl-2-piperidino-benzyl) carbamoyl]methyl] benzoic acid, a substituted benzoic acid with an asymmetric carbon atom. 2. At a non-stimulatory concentration of gluc...

journal_title：British journal of pharmacology

authors： Garrino MG,Henquin JC

更新日期：1988-01-01 00:00:00

abstract：:1. The distribution of sympathetic adrenergic nerves on the rat middle cerebral artery and on the arterioles which originated from it was determined by use of gloxylic histochemistry. 2. Whereas the middle cerebral artery and proximal arterioles arising from this artery received a sympathetic innervation, the distal r...

journal_title：British journal of pharmacology

authors： Edwards FR,Hards D,Hirst GD,Silverberg GD

更新日期：1989-04-01 00:00:00

abstract：:The chemical trimethylcyclohexanol (TMC) is closely related to menthol, the major component of a terpene preparation with known choleretic and cholelitholytic activity. Its effects on hepatic cholesterol synthesis and bile secretion were examined in the rat. In both acute and long-term dosing experiments TMC significa...

journal_title：British journal of pharmacology

authors： Bell GD,Clegg RJ,Ellis WR,Middleton B,White DA

更新日期：1984-01-01 00:00:00

abstract：:The effects of 10 mM caffeine (CAF) on intramembrane charge movements (ICM) were studied in isolated guinea-pig ventricular heart cells with the whole-cell patch-clamp technique. In the presence of CAF, the properties (voltage dependence, maximum Q(ON) [Q(max)], availability with voltage) of Q(ON) charge activated fro...

journal_title：British journal of pharmacology

authors： Leroy J,Lignon JM,Gannier F,Argibay JA,Malécot CO

更新日期：2002-02-01 00:00:00

abstract：:Muscularis mucosa of the distal oesophagus of the opossum contains nerves which release acetylcholine and substance P(SP)-like material on field stimulation. The release of SP-like material appeared to be inhibited by the presence of exogenous muscarinic agonists and potentiated by muscarinic antagonists. Analysis of ...

journal_title：British journal of pharmacology

authors： Daniel EE,Jury J,Robotham KH

更新日期：1986-07-01 00:00:00

abstract：:1 Picrotoxin selectively and reversibly suppressed the inhibitory action of gamma-aminobutyric acid (GABA), but not that of glycine, taurine or beta-alanine, on the frequency of spontaneous spike discharges in guinea-pig cerebellar slices. Strychnine reversibly suppressed the inhibitory action of glycine, taurine or b...

journal_title：British journal of pharmacology

authors： Okamoto K,Quastel JH

更新日期：1976-05-01 00:00:00

abstract：:1. Two preparations, a segment of the ileum and the myenteric plexuslongitudinal muscle preparation, have been used for an analysis of the inhibitory effects of adrenaline, noradrenaline and isoprenaline on the contractor responses of the longitudinal muscle to acetylcholine or to electrical, coaxial or field, stimula...

journal_title：British journal of pharmacology

authors： Kosterlitz HW,Lydon RJ,Watt AJ

更新日期：1970-06-01 00:00:00

abstract：:1. The pharmacological profile of LR-B/081, (methyl 2-[[4-butyl-2-methyl- 6-oxo-5-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1(6H)- pyrimidinyl]methyl]-3-thiophenecarboxylate), a novel antagonist at the angiotensin II (AII) AT1-receptor, was studied in vitro and in vivo. 2. In rabbit aortic strips incubated w...

journal_title：British journal of pharmacology

authors： Cirillo R,Renzetti AR,Cucchi P,Guelfi M,Salimbeni A,Caliari S,Castellucci A,Evangelista S,Subissi A,Giachetti A

更新日期：1995-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is growing evidence that inflammation plays a major role in the pathogenesis of neural damage caused by deposition of amyloid β (Aβ) in the brain. Nimodipine has received attention as a drug that might improve learning and reduce cognitive deficits in Alzheimer's disease, but the mechanism ...

journal_title：British journal of pharmacology

authors： Sanz JM,Chiozzi P,Colaianna M,Zotti M,Ferrari D,Trabace L,Zuliani G,Di Virgilio F

更新日期：2012-12-01 00:00:00

abstract：:1. The purpose of the present investigations was to determine the influence of increasing age on the pharmacokinetics and pharmacodynamics of midazolam in male BN/BiRij rats as an animal model of aging. 2. Midazolam was administered intravenously at a dose of 2.5 mg kg-1 and its pharmacokinetics were determined on the...

journal_title：British journal of pharmacology

authors： Hovinga S,Stijnen AM,Langemeijer MW,Mandema JW,van Bezooijen CF,Danhof M

更新日期：1992-09-01 00:00:00

abstract：:1 The actions of prostaglandin F2 alpha (PGF2 alpha) and noradrenaline on contraction and 45Ca exchange have been studied in rat mesenteric arteries. 2 PGF2 alpha and noradrenaline contracted rat isolated mesenteric artery preparations to about the same extent. The PGF2 alpha-stimulated contractions, unlike those prod...

journal_title：British journal of pharmacology

authors： Godfraind T,Miller RC

更新日期：1982-01-01 00:00:00

abstract：:1 PD 117302, a new nonpeptide opioid compound shown in in vitro studies to be a selective kappa-opioid agonist, has been evaluated in vivo for antinociceptive activity and other effects characteristic of kappa-receptor activation. 2 Dose-related long lasting antinociception was produced by PD 117302 against a mechanic...

journal_title：British journal of pharmacology

authors： Leighton GE,Johnson MA,Meecham KG,Hill RG,Hughes J

更新日期：1987-12-01 00:00:00

abstract：:1. Hypercholesterolaemia often occurs in patients with type 2 diabetes, who therefore encounter administration of HMG-CoA reductase inhibitors. Alteration of pancreatic beta-cell function leading to an impaired insulin secretory response to glucose plays a crucial role in the pathogenesis of type 2 diabetes. Therefore...

journal_title：British journal of pharmacology

authors： Yada T,Nakata M,Shiraishi T,Kakei M

更新日期：1999-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:K(v)11.1 channels are involved in regulating cellular excitability in various tissues including brain, heart and smooth muscle. In these tissues, at least two isoforms, K(v)11.1a and K(v)11.1b, with different kinetics, are expressed. K(v)11.1 activators are potential therapeutic agents, but their...

journal_title：British journal of pharmacology

authors： Larsen AP,Bentzen BH,Grunnet M

更新日期：2010-10-01 00:00:00

abstract：:1. The effects of diprafenone and propafenone on transmembrane action potential were examined and compared in papillary muscles and single ventricular myocytes isolated from guinea-pig hearts. 2. In papillary muscles, both diprafenone and propafenone > or = 10(-6) M caused a significant and dose-dependent decrease in ...

journal_title：British journal of pharmacology

authors： Kodama I,Suzuki R,Honjo H,Toyama J

更新日期：1992-11-01 00:00:00

abstract：:1. It has previously been shown that the antimigraine drug sumatriptan constricts porcine carotid arteriovenous anastomoses via 5-HT1-like receptors, identical to 5-H1B/1D receptors. The recent availability of silent antagonists selective for the 5-HT1B (SB224289) and 5-HT1D (BRL15572) receptor led us to further analy...

journal_title：British journal of pharmacology

authors： De Vries P,Willems EW,Heiligers JP,Villalón CM,Saxena PR

更新日期：1999-05-01 00:00:00

abstract：:1. In a first series of experiments, male Long Evans rats were chronically instrumented for the measurement of internal carotid blood flow and systemic arterial blood pressure; cardiovascular changes were assessed during and after 30 min infusions of human alpha-calcitonin gene-related peptide (CGRP) (0.06 and 0.6 nmo...

journal_title：British journal of pharmacology

authors： Gardiner SM,Compton AM,Bennett T,Kemp PA,Ney U

更新日期：1990-04-01 00:00:00

abstract：:Relaxin is a small heterodimeric peptide hormone of the insulin/relaxin superfamily produced mainly in female and male reproductive organs. It has potent antifibrotic, vasodilatory and angiogenic effects and regulates the normal function of various physiological systems. Preclinical studies and recent clinical trials ...

journal_title：British journal of pharmacology

authors： Agoulnik AI,Agoulnik IU,Hu X,Marugan J

更新日期：2017-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inflammation associated with the tumour microenvironment (TME) plays a critical role in the cancer development, and immunotherapeutic strategies that aim to modulate the immune response in cancer have been crucial. In this study, a Methotrexate-loaded (MTX) poly (lactic-co-glycolic acid)-based (P...

journal_title：British journal of pharmacology

authors： Cavalcante RS,Ishikawa U,Silva ES,Silva Júnior AA,Araújo AA,Cruz LJ,Chan AB,Araújo Júnior RF

更新日期：2021-01-12 00:00:00