Trigeminal antidromic vasodilatation and plasma extravasation in the rat: effects of acetylcholine antagonists and cholinesterase inhibitors.

abstract：:1. In the present paper, we describe the in vitro pharmacological properties of LF 16.0335 (1-[[3-[(2,4-dimethylquinolin-8-yl)oxymethyl]-2,4-dichloro-p henyl]sulphonyl] -2(S) - [[4 -[4-(aminoiminomethyl)phenylcarbonyl]piperazin-1-yl]ca rbonyl]pyrrolidine), a novel and potent nonpeptide antagonist of the human bradykin...

journal_title：British journal of pharmacology

authors： Pruneau D,Luccarini JM,Fouchet C,Defrêne E,Franck RM,Loillier B,Duclos H,Robert C,Cremers B,Bélichard P,Paquet JL

更新日期：1998-09-01 00:00:00

abstract：:1 The effect of intrarenal histamine, dimaprit (H2-agonist) and 2-(2-pyridyl) ethylamine (H1-agonist) on renin release was examined in anaesthetized dogs. 2 In dogs with intact kidneys, histamine and dimaprit administration resulted in renal vasodilatation, a two fold increase in urinary sodium excretion, and no chang...

journal_title：British journal of pharmacology

authors： Gerber JG,Nies AS

更新日期：1983-05-01 00:00:00

abstract：:1 Histamine produced dose-dependent contractile responses on both isolated perfused ear arteries and aortic strips of the rabbit. These responses were blocked by mepyramine and potentiated by both metiamide and dithiothreitol. 2 In the presence of maximum potentiation by metiamide, dithiothreitol still potentiated the...

journal_title：British journal of pharmacology

authors： Carroll PR,Glover WE

更新日期：1977-02-01 00:00:00

abstract：:The aims of this study were to develop a technique to measure blood flow in the mouse ear and to investigate the nature of the vasodilator mediator(s) involved in the response to capsaicin. The response to capsaicin, applied topically, was investigated in anaesthetized CD1 or Sv129+C57BL/6 wild-type (+/+) or NK(1) rec...

journal_title：British journal of pharmacology

authors： Grant AD,Gerard NP,Brain SD

更新日期：2002-01-01 00:00:00

abstract：:1 Inactivation of prostaglandin E2 in the pulmonary circulation of rabbits in vivo was measured by comparing the hypotensive effects of doses given intravenously and intra-arterially. 2 Di-4-phloretin phosphate (DPP) 25-100 mug kg-1 min-1 inhibited the inactivation of prostaglandin E2 in the pulmonary circulation. 3 T...

journal_title：British journal of pharmacology

authors： Crutchley DJ,Piper PJ

更新日期：1975-07-01 00:00:00

abstract：:BACKGROUND AND PURPOSE The transepithelial absorption of Na(+) in the lungs is crucial for the maintenance of the volume and composition of epithelial lining fluid. The regulation of Na(+) transport is essential, because hypo- or hyperabsorption of Na(+) is associated with lung diseases such as pulmonary oedema or cys...

journal_title：British journal of pharmacology

authors： Althaus M,Urness KD,Clauss WG,Baines DL,Fronius M

更新日期：2012-07-01 00:00:00

abstract：:1. The receptor for glucagon-like peptide-1 (GLP-1) can be activated by both its physiological hormone and a peptide discovered in the venom of the Gila Monster, exendin-4, which shows promise as an antidiabetic agent. 2. Exendin-4 displays receptor-binding properties not observed for GLP-1. Firstly, exendin-4 can be ...

journal_title：British journal of pharmacology

authors： Al-Sabah S,Donnelly D

更新日期：2003-09-01 00:00:00

abstract：:1. In cultured endothelial cells of the pig the endothelium-derived relaxing factor (EDRF) releasing agent thrombin (2 u ml-1) caused a significant increase in basal levels of both guanosine 3':5'-cyclic monophosphate (cyclic GMP) and inositol 1,4,5-trisphosphate (IP3). This increase was time dependent, with peak leve...

journal_title：British journal of pharmacology

authors： Lang D,Lewis MJ

更新日期：1991-01-01 00:00:00

abstract：:Extensive in vitro and in vivo studies have shown that cannabinoid drugs have neuroprotective properties and suggested that the endocannabinoid system may be involved in endogenous neuroprotective mechanisms. On the other hand, neurotoxic effects of cannabinoids in vitro and in vivo were also described. Several possib...

journal_title：British journal of pharmacology

authors： Sarne Y,Asaf F,Fishbein M,Gafni M,Keren O

更新日期：2011-08-01 00:00:00

abstract：:I.c.v. self-administration of MDMA (0.01-2 micro g per infusion), alone and in combination with CP 55,940 (0.4 micro g infusion(-1)), was studied on an operant responding procedure. On the basis of individual preference for one of two levers, developed during training, rats were allowed to self-administer vehicle from...

journal_title：British journal of pharmacology

authors： Braida D,Sala M

更新日期：2002-08-01 00:00:00

abstract：:1. Enprostil is composed, in approximately equal proportions, of 4 allenic isomers which are prostanoids structurally related to prostaglandin E2 (PGE2). The isomers are denoted as RS-86505-007, RS-86812-007 which are in the 'natural' R and S configuration (with respect to PGE2) and RS-86505-008 and RS-86812-008 which...

journal_title：British journal of pharmacology

authors： Eglen RM,Whiting RL

更新日期：1989-12-01 00:00:00

abstract：:Two prostaglandin endoperoxide analogues, EP 035 and EP 157, behave as specific thromboxane receptor antagonists on isolated smooth muscle preparations such as rabbit aorta, dog saphenous vein and guinea-pig trachea. However, in human platelet-rich plasma (PRP) they produce an unsurmountable block of aggregation induc...

journal_title：British journal of pharmacology

authors： Armstrong RA,Jones RL,MacDermot J,Wilson NH

更新日期：1986-03-01 00:00:00

abstract：:Peroxisome proliferator activated receptors (PPAR)s are nuclear transcription factors of the steroid receptor super-family. One member, PPARgamma, a critical transcription factor in adipogenesis, is expressed in ECV304 cells, and when activated participates in the induction of cell death by apoptosis. Here we describe...

journal_title：British journal of pharmacology

authors： Bishop-Bailey D,Hla T,Warner TD

更新日期：2000-10-01 00:00:00

abstract：:1. In many cancer patients, 5-fluorouracil (5-FUra) treatment is toxic and even causes death. Nevertheless, all patients are subjected to a standard therapy regimen because there is no reliable way to identify beforehand those patients who are predisposed to 5-FUra-induced toxicity. In this study, we identified the di...

journal_title：British journal of pharmacology

authors： Jiang H,Lu J,Ji J

更新日期：2004-02-01 00:00:00

abstract：:The pharmacological properties of fatty acid amidohydrolase (FAAH) were investigated in brains of 35-day-old chickens, since nothing is known about the enzyme in avian species. FAAH activity towards both [(3)H]-palmitoylethanolamide (PEA) [K(M)=1.5 microM] and [(3)H]-anandamide (AEA) [K(M)=5.4 microM] was demonstrated...

journal_title：British journal of pharmacology

authors： Fowler CJ,Börjesson M,Tiger G

更新日期：2000-10-01 00:00:00

abstract：:A method is described for the determination of halothane-induced sleeping time in the rat. 2 The sleeping time exhibited a diurnal variation which was due, at least in part, to a change in the sensitivity of the central nervous system (CNS) to the anaesthetic. 3 Tolerance to halothane did not develop in rats repeatedl...

journal_title：British journal of pharmacology

authors： Turnbull MJ,Watkins JW

更新日期：1976-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Exposure to an acute stress inhibits gastric emptying and stimulates colonic transit via central neuropeptide Y (NPY) pathways; however, peripheral involvement is uncertain. The anxiogenic phenotype of NPY(-/-) mice is gender-dependent, raising the possibility that stress-induced gastrointestinal...

journal_title：British journal of pharmacology

authors： Forbes S,Herzog H,Cox HM

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Screening of 12,000 compounds for binding affinity to the synaptic vesicle protein 2A (SV2A), identified a high-affinity pyrrolidone derivative, brivaracetam (ucb 34714). This study examined its pharmacological profile in various in vitro and in vivo models of seizures and epilepsy, to evaluate i...

journal_title：British journal of pharmacology

authors： Matagne A,Margineanu DG,Kenda B,Michel P,Klitgaard H

更新日期：2008-08-01 00:00:00

abstract：:1 A procedure involving two guinea-pig isolated hearts perfused in series is described for detecting in the recipient heart the release of a possible coronary vasodilator metabolite from the donor heart. 2 Adrenaline and isoprenaline stimulated the rate and force of contraction and produced a multiphasic coronary vasc...

journal_title：British journal of pharmacology

authors： Broadley KJ

更新日期：1976-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Caffeine is one of the most commonly used psychoactive substances. Circadian rhythms consist of the main suprachiasmatic nucleus (SCN) clocks and peripheral clocks. Although caffeine lengthens circadian rhythms and modifies phase changes in SCN-operated rhythms, the effects on caffeine on the pha...

journal_title：British journal of pharmacology

authors： Narishige S,Kuwahara M,Shinozaki A,Okada S,Ikeda Y,Kamagata M,Tahara Y,Shibata S

更新日期：2014-12-01 00:00:00

abstract：:For almost three decades intrathecal baclofen therapy has been the standard treatment for spinal cord injury spasticity when oral medication is ineffective or produces serious side effects. Although intrathecal baclofen therapy has a good clinical benefit-risk ratio for spinal spasticity, tolerance and the life-threat...

journal_title：British journal of pharmacology

authors： Gómez-Soriano J,Goiriena E,Taylor J

更新日期：2010-11-01 00:00:00

abstract：:1. The effect of the calcitonin gene-related peptide antagonist (CGRP8-37, 400 nmol kg-1, i.v.) on the increased blood flow induced by calcitonin gene related peptide (CGRP), vasodilator prostaglandins, and topical capsaicin was measured with a laser Doppler blood flow meter in rat abdominal skin. 2. The saphenous ner...

journal_title：British journal of pharmacology

authors： Escott KJ,Brain SD

更新日期：1993-10-01 00:00:00

abstract：:1,1-Azobis[3-methyl-2-phenylbenzimidazolinium]dimethanesulphonate (AH 10407) has an ultrashort, competitive neuromuscular blocking action in the mouse, cat, dog, Cynamolgus monkey and cotton-eared marmoset. 2 AH 10407 is chemically unstable in bicarbonate-containing solutions and is degraded to inactive products. The ...

journal_title：British journal of pharmacology

authors： Brittain RT,Jack D,Tyers MB

更新日期：1977-09-01 00:00:00

abstract：:Data presentation and statistical analysis in scientific writing are agreed to be in need of improvement, despite the profusion of advice and instruction. Recent evidence supports the need for better planning and analysis of animal experiments. This series of short articles aims to provide advice in small easily diges...

journal_title：British journal of pharmacology

authors： Drummond GB,Vowler SL

更新日期：2011-05-01 00:00:00

abstract：:1. In cortical slices from rat brain incubated in a medium containing the irreversible cholinesterase inhibitor, soman (0.005 mM) and a high concentration of KCl (25 mM), atropine exerts a stimulating action on the release of acetylcholine (ACh).2. Two possible explanations for this action were examined. Atropine migh...

journal_title：British journal of pharmacology

authors： Polak RL

更新日期：1971-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Due to their potent bronchodilator properties, beta(2)-adrenoceptor agonists are a mainstay of therapy in asthma. However, the effects of beta(2)-adrenoceptor agonists on inflammation are less clear. Accordingly, we have investigated the effects of beta(2)-adrenoceptor agonists on inflammatory me...

journal_title：British journal of pharmacology

authors： Holden NS,Rider CF,Bell MJ,Velayudhan J,King EM,Kaur M,Salmon M,Giembycz MA,Newton R

更新日期：2010-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The rat respiratory muscle diaphragm has markedly lower sensitivity than the locomotor muscle extensor digitorum longus (EDL) to the new acetylcholinesterase (AChE) inhibitors, alkylammonium derivatives of 6-methyluracil (ADEMS). This study evaluated several possible reasons for differing sensiti...

journal_title：British journal of pharmacology

authors： Petrov KA,Yagodina LO,Valeeva GR,Lannik NI,Nikitashina AD,Rizvanov AA,Zobov VV,Bukharaeva EA,Reznik VS,Nikolsky EE,Vyskočil F

更新日期：2011-06-01 00:00:00

abstract：:1. The uptake of (3)H-digitoxin, (3)H-ouabain and (3)H-dihydro-ouabain by isolated guinea-pig atria has been studied and compared with the inhibition of the sodium pump and with the inotropic effect.2. Analysis of the curve relating the uptake of digitoxin and ouabain at equilibrium to the bath concentration enabled a...

journal_title：British journal of pharmacology

authors： Godfraind T,Lesne M

更新日期：1972-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gain of function mutations in TRPC6 channels can cause autosomal dominant forms of focal segmental glomerulosclerosis (FSGS). Validated inhibitors of TRPC6 channels that are biologically active on FSGS-related TRPC6 mutants are eagerly sought. EXPERIMENTAL APPROACH:We synthesized new TRPC6-inhib...

journal_title：British journal of pharmacology

authors： Urban N,Neuser S,Hentschel A,Köhling S,Rademann J,Schaefer M

更新日期：2017-11-01 00:00:00

abstract：:The administration of arachidonic acid (AA) to the isolated perfused heart of the rat usually produced biphasic coronary responses characterized by initial vasoconstriction followed by prolonged vasodilatation. However, some responses were predominantly vasoconstrictor or vasodilator. The non-steroidal anti-inflammato...

journal_title：British journal of pharmacology

authors： Belo SE,Talesnik J

更新日期：1982-02-01 00:00:00