Studies on RX 781094: a selective, potent and specific antagonist of alpha 2-adrenoceptors.

abstract：:The inhibitory effects of three prostanoid analogues, EP 045, EP 092 and pinane thromboxane A2 (PTA2), on the aggregation of human platelets in vitro have been investigated. In diluted platelet-rich plasma (PRP), EP 045 (20 microM) and EP 092 (1 microM) completely inhibited irreversible aggregation responses to thromb...

journal_title：British journal of pharmacology

authors： Armstrong RA,Jones RL,Peesapati V,Will SG,Wilson NH

更新日期：1985-03-01 00:00:00

abstract：:1. The effect on membrane currents of infection of mouse neuroblastoma NA cells with rabies virus was studied by using the whole-cell patch clamp technique. 2. Three types of membrane currents, namely voltage-dependent Na+ current (I(Na)), delayed rectifier K+ current (I(K-DR)) and inward rectifier K+ current (I(K-IR)...

journal_title：British journal of pharmacology

authors： Iwata M,Komori S,Unno T,Minamoto N,Ohashi H

更新日期：1999-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Activation of cannabinoid receptors decreases emesis, inflammation, gastric acid secretion and intestinal motility. The ability to modulate intestinal permeability in inflammation may be important in therapy aimed at maintaining epithelial barrier integrity. The aim of the present study was to de...

journal_title：British journal of pharmacology

authors： Alhamoruni A,Wright KL,Larvin M,O'Sullivan SE

更新日期：2012-04-01 00:00:00

abstract：:1 We investigated the peripheral haemodynamic effects of human alpha-calcitonin gene-related peptide (CGRP) following administration of endothelin-1 or NG-nitro-L-arginine methyl ester (L-NAME), an inhibitor of nitric oxide production, in conscious, chronically-instrumented, Long Evans rats. 2 Infusion of endothelin-1...

journal_title：British journal of pharmacology

authors： Gardiner SM,Compton AM,Kemp PA,Bennett T,Foulkes R,Hughes B

更新日期：1991-05-01 00:00:00

abstract：:Prostate cancer is the second most common malignancy in men and androgen deprivation therapy is the first-line therapy. However, most cases will eventually develop castration-resistant prostate cancer after androgen deprivation therapy treatment. Enzalutamide is a second-generation androgen receptor antagonist approve...

journal_title：British journal of pharmacology

authors： Wang Y,Chen J,Wu Z,Ding W,Gao S,Gao Y,Xu C

更新日期：2020-11-05 00:00:00

abstract：:The endogenous concentrations of p- and m-hydroxyphenylacetic acid in the mouse caudate nucleus were determined by a gas chromatographic or a gas chromatographic-mass spectrometric technique and the concentrations were about 30 and 11 ng g-1 respectively. The subcutaneous administration of (+)-butaclamol (1 mg kg-1), ...

journal_title：British journal of pharmacology

authors： Juorio AV,McQuade PS

更新日期：1983-11-01 00:00:00

abstract：:1. Prostaglandin F2 alpha (PGF2 alpha) and its synthetic analogue, fluprostenol, potently relaxed the precontracted isolated jugular vein of the rabbit (RJuV). The vasorelaxant activity of PGF2 alpha and fluprostenol was dependent upon an intact vascular endothelium. Although removal of the vascular endothelium abolis...

journal_title：British journal of pharmacology

authors： Chen J,Champa-Rodriguez ML,Woodward DF

更新日期：1995-12-01 00:00:00

abstract：:The aim of the present study was to determine whether inhibition of cyclic nucleotide phosphodiesterase (PDE) modulates the stimulated generation of the cytokines, interleukin-4 (IL-4) and IL-13, from human basophils. This was addressed by evaluating the effects of both nonselective and selective inhibitors of PDEs on...

journal_title：British journal of pharmacology

authors： Eskandari N,Wickramasinghe T,Peachell PT

更新日期：2004-08-01 00:00:00

abstract：:The effect of fluoxetine on uptake of 5-hydroxytryptamine (5-HT) by enteric 5-hydroxytryptaminergic neurones has been analyzed in order to compare further these neurones with 5-HT neurones of the CNS. In addition, the effects of fluoxetine and chlorimipramine on efflux of [3H]-5-HT from the myenteric plexus were also ...

journal_title：British journal of pharmacology

authors： Gershon MD,Jonakait GM

更新日期：1979-05-01 00:00:00

abstract：:1. We have studied the effect of cannabinoid agonists (CP 55,940 and cannabinol) on intestinal motility in a model of intestinal inflammation (induced by oral croton oil in mice) and measured cannabinoid receptor expression, endocannabinoids (anandamide and 2-arachidonylglycerol) and anandamide amidohydrolase activity...

journal_title：British journal of pharmacology

authors： Izzo AA,Fezza F,Capasso R,Bisogno T,Pinto L,Iuvone T,Esposito G,Mascolo N,Di Marzo V,Capasso F

更新日期：2001-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The Rho GTPase, Rac1, is involved in the pathogenesis of neuropathic pain induced by malformation of dendritic spines in the spinal dorsal horn (sDH) neurons. In the present study, the contribution of spinal Rac1 to peripheral inflammatory pain was studied. EXPERIMENTAL APPROACH:Effects of s.c. ...

journal_title：British journal of pharmacology

authors： Wang Y,Lu YF,Li CL,Sun W,Li Z,Wang RR,He T,Yang F,Yang Y,Wang XL,Guan SM,Chen J

更新日期：2016-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Agmatine, a putative neurotransmitter, plays a vital role in learning and memory. Although it is considered an endogenous ligand of imidazoline receptors, agmatine exhibits high affinity for α-adrenoceptors, NOS and NMDA receptors. These substrates within the locus coeruleus (LC) are critically i...

journal_title：British journal of pharmacology

authors： Shelkar GP,Gakare SG,Chakraborty S,Dravid SM,Ugale RR

更新日期：2016-09-01 00:00:00

abstract：:1. In the rat isolated diaphragm preparation hexamethonium and other low potency competitive antagonists of acetylcholine (ACh), including gallamine and hyoscine butylbromide, reverse block by the potent antagonists tubocurarine, pancuronium and alcuronium. 2. In the presence of tubocurarine, hexamethonium increases t...

journal_title：British journal of pharmacology

authors： Blackman JG,Gauldie RW,Milne RJ

更新日期：1975-05-01 00:00:00

abstract：:1 Administration of isoprenaline by aerosol inhalation to man results in over 80% being metabolized to the sulphate conjugate.2 The majority of an inhaled dose is probably swallowed since the metabolic pattern resembles that after an oral dose.3 Isoprenaline, administered in aqueous solution directly into the bronchia...

journal_title：British journal of pharmacology

authors： Blackwell EW,Briant RH,Conolly ME,Davies DS,Dollery CT

更新日期：1974-04-01 00:00:00

abstract：:1 The effect of methylene, thio, and imido substituted analogues of adenosine 5'-triphosphate (ATP) on surfactant phospholipid secretion and calcium mobilization in rat isolated alveolar Type II cells was studied. 2 ATP was the most potent secretagogue of adenine nucleotides studied. The rank order of agonist potency ...

journal_title：British journal of pharmacology

authors： Rice WR,Singleton FM

更新日期：1987-08-01 00:00:00

abstract：:1. The affinities of a number of alpha 1-adrenoceptor antagonists were determined by displacement of [3H]-prazosin binding from cloned human alpha 1A-adrenoceptors (previously designated cloned alpha 1c subtype), alpha 1B alpha 1D and rat alpha 1D-adrenoceptors, stably expressed in rat-1 fibroblasts. Functional affini...

journal_title：British journal of pharmacology

authors： Kenny BA,Chalmers DH,Philpott PC,Naylor AM

更新日期：1995-07-01 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 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：: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 Very highly purified (greater than 100,000 u/mg) slow reacting substance of anaphylaxis (SRS-A) has been prepared by reversed phase high pressure liquid chromatographic (HPLC) techniques. 2 High resolution liquid chromatography suggests that SRS-A may exist in at least three distinct forms which are possible tautome...

journal_title：British journal of pharmacology

authors： Blackwell GJ,Burka JF,Flower RJ,Torkington P

更新日期：1980-01-01 00:00:00

abstract：:1. The polymorphonuclear neutrophils (PMN) activation and mobilization observed in acute cerebral infarction contribute to the brain tissue damage, but PMN could also be involved in postischemic functional injury of ischemied blood vessel. 2. This study was undertaken to investigate whether pharmacological neutropenia...

journal_title：British journal of pharmacology

authors： Pétrault O,Ouk T,Gautier S,Laprais M,Gelé P,Bastide M,Bordet R

更新日期：2005-04-01 00:00:00

abstract：:1. The effects of cocaine, 6-hydroxydopamine (6-OHDA), reserpine and 17-beta-oestradiol on the sensitivity of the rat anococcygeus muscle to noradrenaline (NA), acetylcholine (ACh) and KCl were investigated.2. Cocaine (10(-5)M) increased the sensitivity of the anococcygeus to NA (100-fold) but not to ACh or KCl.3. 6-O...

journal_title：British journal of pharmacology

authors： Gibson A,Pollock D

更新日期：1973-11-01 00:00:00

abstract：:Immersion of the hind paws of anesthetized rats in hot water for 5 min induced massive plasma protein leakage as indicated by extravasation of Evans blue dye in the skin. The threshold temperature which caused noticeable plasma extravasation was 45 degrees C, a maximal response was obtained between 55 degrees C and 60...

journal_title：British journal of pharmacology

authors： Saria A

更新日期：1984-05-01 00:00:00

abstract：:1. Behavioural activity (delayed differentiation and spatial delayed alternation) and pharmacokinetics of diazepam and its metabolites, N-desmethyldiazepam (nordiazepam), 3-hydroxydiazepam (temazepam) and 3-hydroxy-N-desmethyldiazepam (oxazepam), and of dipotassium clorazepate (clorazepate), were studied in the monkey...

journal_title：British journal of pharmacology

authors： Curry SH,Whelpton R,Nicholson AN,Wright CM

更新日期：1977-11-01 00:00:00

abstract：:1. The GABA-B receptor agonists baclofen and 3-aminopropylphosphinic acid (3-APPi) have antitussive activity in the cat and guinea pig. The purpose of this study was to investigate the sites of action of these GABA-B receptor agonists to inhibit the cough reflex. 2. Single intracerebroventricular (i.c.v.) cannulas wer...

journal_title：British journal of pharmacology

authors： Bolser DC,DeGennaro FC,O'Reilly S,Chapman RW,Kreutner W,Egan RW,Hey JA

更新日期：1994-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Previous findings suggest that the growth and differentiation factor midkine (Mdk) is a negative regulator of osteoblast activity and bone formation, thereby raising the possibility that a specific Mdk antagonist might improve bone formation during fracture healing. EXPERIMENTAL APPROACH:In the ...

journal_title：British journal of pharmacology

authors： Haffner-Luntzer M,Heilmann A,Rapp AE,Roessler R,Schinke T,Amling M,Ignatius A,Liedert A

更新日期：2016-07-01 00:00:00

abstract：:1. The mechanisms underlying the vasodilator response to urocortin are incompletely understood. The present study was designed to examine the role of endothelial nitric oxide and Ba(2+)-sensitive K(+) channels in the endothelium-dependent component of urocortin-induced relaxation in the rat left anterior descending co...

journal_title：British journal of pharmacology

authors： Huang Y,Chan FL,Lau CW,Tsang SY,He GW,Chen ZY,Yao X

更新日期：2002-03-01 00:00:00

abstract：:By implanting a Teflon chamber subcutaneously into a sheep a mild aseptic inflammatory lesion was produced from which wound fluid could be sampled daily. The prostaglandin content of this wound fluid was examined. Prostaglandin E2 activity was found in all samples, and a peak was apparent on the fourth or fifth day af...

journal_title：British journal of pharmacology

authors： Greenwood B,Kerry PJ

更新日期：1975-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

journal_title：British journal of pharmacology

authors： Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

更新日期：2015-09-01 00:00:00

abstract：:The platelet-lowering drug anagrelide inhibits bone marrow megakaryocytopoiesis by an unknown mechanism. Recently, it was found that anagrelide is bio-transformed in humans into two major metabolites (6,7-dichloro-3-hydroxy-1,5 dihydro-imidazo[2,1-b]quinazolin-2-one (BCH24426) and 2-amino-5,6-dichloro-3,4,-dihydroquin...

journal_title：British journal of pharmacology

authors： Wang G,Franklin R,Hong Y,Erusalimsky JD

更新日期：2005-10-01 00:00:00