Effect of 781094, a new selective alpha-adrenoceptor antagonist, on the aggregatory responses of human blood platelets and on binding of [3H]-dihydroergocryptine to these cells.

abstract：UNLABELLED:Cell movement is a fundamental process of normal cellular physiology and pathophysiology. Abnormal regulation of cell migration is a common denominator of many medical disorders, including cancer metastasis, autoimmune disease and inflammation. Increased interest in the targeting of cell migration and invasi...

journal_title：British journal of pharmacology

authors： Detchokul S,Frauman AG

更新日期：2014-12-01 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：:Chronic itch poses major health care and economic burdens worldwide. In 2013, B-type natriuretic peptide (BNP) was identified as an itch-selective neuropeptide and shown to be both necessary and sufficient to produce itch behaviour in mice. Since then, mechanistic studies of itch have increased, not only at central le...

journal_title：British journal of pharmacology

authors： Meng J,Chen W,Wang J

更新日期：2020-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The effects of systemic treatment with indomethacin-loaded nanocapsules (IndOH-NC) were compared with those of free indomethacin (IndOH) in rat models of acute and chronic oedema. EXPERIMENTAL APPROACH:The following models of inflammation were employed: carrageenan-induced acute oedema (measured...

journal_title：British journal of pharmacology

authors： Bernardi A,Zilberstein AC,Jäger E,Campos MM,Morrone FB,Calixto JB,Pohlmann AR,Guterres SS,Battastini AM

更新日期：2009-10-01 00:00:00

abstract：:1. Effects of neuropeptides of the vasopressin family on Cl(-) secretion have not yet been reported in lung. Using the 16HBE14o- bronchial epithelial cell line, we investigated their action on Cl(-) secretion. 2. In symmetrical Cl(-) solutions, basolateral application of arginine vasotocin (AVT), oxytocin or isotocin ...

journal_title：British journal of pharmacology

authors： Bernard K,Bogliolo S,Ehrenfeld J

更新日期：2005-04-01 00:00:00

abstract：:Athletes attempt to improve performance with drugs that act on the beta-adrenergic system directly or indirectly. Of three beta-adrenoceptor (AR) subtypes, the beta(2)-AR is the main target in sport; they have bronchodilator and anabolic actions and enhance anti-inflammatory actions of corticosteroids. Although demons...

journal_title：British journal of pharmacology

authors： Davis E,Loiacono R,Summers RJ

更新日期：2008-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-arachidonoyl-serotonin (AA-5-HT) is an inhibitor of fatty acid amide hydrolase (FAAH)-catalysed hydrolysis of the endocannabinoid/ endovanilloid compound, anandamide (AEA). We investigated if AA-5-HT antagonizes the transient receptor potential vanilloid-1 (TRPV1) channel and, as FAAH and TRPV1...

journal_title：British journal of pharmacology

authors： Maione S,De Petrocellis L,de Novellis V,Moriello AS,Petrosino S,Palazzo E,Rossi FS,Woodward DF,Di Marzo V

更新日期：2007-03-01 00:00:00

abstract：:Rats were placed on either a low sodium intake (low sodium diet 0.025% dry weight, tap water for drinking) or a high sodium intake (normal sodium diet 0.45% dry weight, 0.9% saline for drinking) for 10 days. The pressor-response curve to angiotensin II in rats previously on a high sodium intake was shifted to the left...

journal_title：British journal of pharmacology

authors： Jones DR,Penner SB,Smyth DD

更新日期：1985-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Subunit-specific modulators of gamma-aminobutyric acid (GABA) type A (GABA(A)) receptors can help to assess the physiological function of receptors with different subunit composition and also provide the basis for the development of new drugs. Valerenic acid (VA) was recently identified as a beta...

journal_title：British journal of pharmacology

authors： Khom S,Strommer B,Ramharter J,Schwarz T,Schwarzer C,Erker T,Ecker GF,Mulzer J,Hering S

更新日期：2010-09-01 00:00:00

abstract：:1 The selectivity and specificity of RX 781094 [2-(2-(1,4 benzodioxanyl))2-imidazoline HCl] for alpha-adrenoceptors have been examined in peripheral tissues. 2 In isolated tissue experiments RX 781094 was a competitive antagonist at prejunctional alpha 2-adrenoceptors situated on the sympathetic nerve terminals of the...

journal_title：British journal of pharmacology

authors： Doxey JC,Roach AG,Smith CF

更新日期：1983-03-01 00:00:00

abstract：:1. We have investigated pre- and post-junctional responsiveness in vas deferens from wild-type and alpha(2A/D)-adrenoceptor knockout mice. The response to a single stimulus was not significantly different between wild-type and knock-out mice. The isometric contraction to 10 Hz stimulation for 4 s was significantly lar...

journal_title：British journal of pharmacology

authors： Cleary L,Vandeputte C,Docherty JR

更新日期：2002-07-01 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：:1. The goal of this study was to determine if an increase in cytoplasmic calcium concentration ([Ca2+]i), in the absence of additional second messengers derived from membrane phospholipid turnover, is a sufficient signal to induce chloride secretion across monolayers of the human colonic epithelial line, T84. 2. Thaps...

journal_title：British journal of pharmacology

authors： Kachintorn U,Vajanaphanich M,Traynor-Kaplan AE,Dharmsathaphorn K,Barrett KE

更新日期：1993-06-01 00:00:00

abstract：:1. The effects of intravenous administration of two alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonists were studied on responses of single neurones to iontophoretically applied excitatory amino acids. The tests were performed on spinal neurones in alpha-chloralose anaesthetized, spinalized rat...

journal_title：British journal of pharmacology

authors： Chizh BA,Cumberbatch MJ,Headley PM

更新日期：1994-07-01 00:00:00

abstract：LINKED ARTICLES:This article is part of a themed section on Recent Progress in the Understanding of Relaxin Family Peptides and their Receptors. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v174.10/issuetoc. ...

journal_title：British journal of pharmacology

authors： Summers RJ

更新日期：2017-05-01 00:00:00

abstract：:1. The effects of 5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) were investigated on evoked and spontaneous currents in freshly-isolated cells from the rat portal vein by use of conventional whole-cell recording and perforated-patch techniques. 2. At a holding potential of -60 mV in potassium-free, caesium-conta...

journal_title：British journal of pharmacology

authors： Kirkup AJ,Edwards G,Weston AH

更新日期：1996-01-01 00:00:00

abstract：:1. The concentrations of adrenaline and noradrenaline in the brains of chickens (Gallus domesticus) have been determined using two different methods of fluorimetric analysis.2. The concentrations of adrenaline, noradrenaline and also dopamine were found to increase with age, as did the relative amount of adrenaline pr...

journal_title：British journal of pharmacology

authors： Callingham BA,Sharman DF

更新日期：1970-09-01 00:00:00

abstract：:Spontaneous inhibitory postsynaptic currents (i.p.s.cs) were recorded in voltage-clamped CA1 neurones in rat hippocampal slices. The exponential decay of i.p.s.cs was prolonged by concentrations of sodium pentobarbitone as low as 50 microM. With concentrations up to 100 microM, there was no change in the amplitude or ...

journal_title：British journal of pharmacology

authors： Gage PW,Robertson B

更新日期：1985-07-01 00:00:00

abstract：:1. A biliary fistula was prepared in twelve sheep.2. Each animal was given 2 ml. of (14)C-carbon tetrachloride (specific activity 15 mc/m-mole) and bile collected at 2, 4, 24 and 48 hr.3. Specific activity was measured by liquid scintillation counting before and after each specimen had been heated to 75 degrees C for ...

journal_title：British journal of pharmacology

authors： Khalidi A,Zaki SA

更新日期：1969-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hypoxia in tumours is known to cause resistance to conventional chemotherapeutic drugs. In contrast, little is known about the effects of hypoxia on targeted anti-cancer drugs. This study evaluated the effect of hypoxia on a series of clinically approved tyrosine kinase inhibitors (TKIs). EXPERI...

journal_title：British journal of pharmacology

authors： Ahmadi M,Ahmadihosseini Z,Allison SJ,Begum S,Rockley K,Sadiq M,Chintamaneni S,Lokwani R,Hughes N,Phillips RM

更新日期：2014-01-01 00:00:00

abstract：:1. The endothelial modulation of the relaxant responses to the nitric oxide (NO) donor sodium nitroprusside (SNP) and the KATP channel opener levcromakalim (LEM) and the interactions between these agents were analysed in isolated rat aorta. 2. LEM-induced relaxation was unchanged by endothelium removal or by the prese...

journal_title：British journal of pharmacology

authors： Pérez-Vizcaíno F,Cogolludo AL,Zaragozá-Arnáez F,Fajardo S,Ibarra M,López-López JG,Tamargo J

更新日期：1999-12-01 00:00:00

abstract：:1. In the present study, the properties of glaucine (an aporphine structurally related to papaverine) were compared with those of papaverine, diltiazem, nifedipine and prazosin. The work includes functional studies on rat isolated aorta contracted with noradrenaline, caffeine or KCl, and a determination of the affinit...

journal_title：British journal of pharmacology

authors： Ivorra MD,Lugnier C,Schott C,Catret M,Noguera MA,Anselmi E,D'Ocon P

更新日期：1992-06-01 00:00:00

abstract：:Human skin fibroblasts incubated with arachidonic acid in culture show basal release of prostaglandins. They produce the same prostaglandins after stimulation with bradykinin. Basal release of prostaglandins I2 (6-oxo-PGF1 alpha), F2 alpha and E2 is inhibited dose-dependently by both acetylsalicylic acid (ASA) and dip...

journal_title：British journal of pharmacology

authors： Lüthy C,Multhaupt M,Oetliker O,Perisic M

更新日期：1983-08-01 00:00:00

abstract：:1. The effects of the metabotropic glutamate receptor (mGluR) antagonist, L-2-amino-3-phosphonopropionate (L-AP3) on phosphoinositide turnover in neonatal rat cerebral cortex slices has been investigated. 2. At concentrations of < or = 300 microM, L-AP3 inhibited total [3H]-inositol phosphate ([3H]-InsPx) and Ins(1,4,...

journal_title：British journal of pharmacology

authors： Mistry R,Prabhu G,Godwin M,Challiss RA

更新日期：1996-03-01 00:00:00

abstract：:1. Previous studies suggested that nitric oxide (NO) may cause hyperpolarization and relaxation of canine colonic smooth muscle by both cGMP-dependent and cGMP-independent mechanisms. This hypothesis was tested using 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline-1-one (ODQ), a novel inhibitor of NO-stimulated guanylate cycla...

journal_title：British journal of pharmacology

authors： Franck H,Sweeney KM,Sanders KM,Shuttleworth CW

更新日期：1997-11-01 00:00:00

abstract：:1. The effects of intradermally injected prostaglandins (PGs) E(1), E(2), F(1alpha) and F(2alpha) have been examined in the rat and in man.2. PGE(1) and PGE(2) caused an increase in local vascular permeability in rat skin; their potency was comparable with that of other putative mediators of inflammation (histamine, b...

journal_title：British journal of pharmacology

authors： Crunkhorn P,Willis AL

更新日期：1971-01-01 00:00:00

abstract：:1 Vasoactive intestinal polypeptide (VIP, 0.01- MicroM) produced dose-related relaxations of the mouse anococcygeus muscle. 2 Following incubation with indomethacin (2.8 microM 1 h) adenosine 5'-triphosphate (ATP, 0.5-10 mM) produced dose-related relaxations of the mouse anococcygeus. 3 Haemolysed blood reduced inhibi...

journal_title：British journal of pharmacology

authors： Gibson A,Tucker JF

更新日期：1982-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Ca(2+)-dependent Cl(-) secretion (CaCC) in airways and other tissues is due to activation of the Cl(-) channel TMEM16A (anoctamin 1). Earlier studies suggested that Ca(2+) -activated Cl(-) channels are regulated by membrane lipid inositol phosphates, and that 1-O-octyl-2-O-butyryl-myo-inositol 3,...

journal_title：British journal of pharmacology

authors： Tian Y,Schreiber R,Wanitchakool P,Kongsuphol P,Sousa M,Uliyakina I,Palma M,Faria D,Traynor-Kaplan AE,Fragata JI,Amaral MD,Kunzelmann K

更新日期：2013-01-01 00:00:00

abstract：:1. A comparative study was carried out to assess the regional haemodynamic effects of intravenous infusion of human alpha- and beta-calcitonin gene-related peptide (CGRP; 0.006, 0.06 and 0.6 nmol h-1) in conscious, unrestrained Wistar rats. 2. With human alpha-CGRP, tachycardia was always accompanied by a fall in mean...

journal_title：British journal of pharmacology

authors： Gardiner SM,Compton AM,Bennett T

更新日期：1989-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Red blood cells (RBCs) are reservoirs of vasodilatory, antiaggregatory, and antiinflammatory lipid mediators-epoxyeicosatrienoic acids (EETs). This study addresses the formation and release of erythrocyte-derived EETs in response to ATP receptor stimulation that may represent an important mechani...

journal_title：British journal of pharmacology

authors： Jiang H,Zhu AG,Mamczur M,Falck JR,Lerea KM,McGiff JC

更新日期：2007-08-01 00:00:00