The action of melatonin on single amphibian pigment cells in tissue culture.

abstract：BACKGROUND AND PURPOSE:A fluorinated derivative (2F-MT-45) of the synthetic μ-opioid receptor agonist MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) was recently identified in a seized illicit tablet. While MT-45 is a Class A drug, banned in a number of countries, nothing is known about the pharmacology of 2F-MT-...

journal_title：British journal of pharmacology

authors： Baptista-Hon DT,Smith M,Singleton S,Antonides LH,Nic Daeid N,McKenzie C,Hales TG

更新日期：2020-08-01 00:00:00

abstract：:1. Effects of phorbol esters on the cytosolic Ca2+ level ([Ca2+]i) and muscle tension in the intestinal smooth muscle of guinea-pig taenia caeci were examined. 2. 12-Deoxyphorbol 13-isobutyrate (DPB, 1 microM) did not change the [Ca2+]i and tension in resting muscle. 3. In high K(+)-stimulated muscle, 1 microM DPB tra...

journal_title：British journal of pharmacology

authors： Mitsui M,Karaki H

更新日期：1993-05-01 00:00:00

abstract：:1. The present experiments were designed to investigate the mechanisms causing intimal hyperplasia in connection with the impaired synergism between prostaglandin I2 (PGI2) and nitric oxide (NO) in human uterine arteries (UAs). 2. In order to assess the magnitude of intimal hyperplasia, the intima:media ratio (%) was ...

journal_title：British journal of pharmacology

authors： Obayashi S,Aso T,Sato J,Hamasaki H,Azuma H

更新日期：1996-11-01 00:00:00

abstract：:1. The series of cycloalcohols C6, C7, C8 and C10 have been used to probe the molecular dimensions of a variety of general anaesthetic target sites. 2. The general anaesthetic EC50 concentrations of the cycloalcohols were determined for tadpoles (Xenopus laevis). All of the cycloalcohols tested were found to be potent...

journal_title：British journal of pharmacology

authors： Curry S,Moss GW,Dickinson R,Lieb WR,Franks NP

更新日期：1991-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Stress is believed to be associated with the development of neuropsychiatric disorders, including Alzheimer's disease (AD). We have studied mechanisms implicated in vulnerability to stress and the relationship with changes in AD-related markers. EXPERIMENTAL APPROACH:Anhedonia induced by a chron...

journal_title：British journal of pharmacology

authors： Briones A,Gagno S,Martisova E,Dobarro M,Aisa B,Solas M,Tordera R,Ramírez M

更新日期：2012-02-01 00:00:00

abstract：:1. Human epicardial coronary artery rings, freshly obtained from cardiac transplant patients, were examined for their responses to endothelium-derived relaxing factor (EDRF)-releasing agents. 2. Functional antagonism profoundly influenced relaxation responses in this tissue. Increasing force with concentrations of U46...

journal_title：British journal of pharmacology

authors： Stork AP,Cocks TM

更新日期：1994-12-01 00:00:00

abstract：:1. The effects of pregnancy on mesenteric arterial function were examined in constantly perfused (5 ml min-1) mesenteric arterial beds isolated from 21-day pregnant rats. The function of sympathetic and sensory-motor perivascular nerves, endothelium and smooth muscle was examined. The role of nitric oxide and prostagl...

journal_title：British journal of pharmacology

authors： Ralevic V,Burnstock G

更新日期：1996-04-01 00:00:00

abstract：:1. The effects of 3 competitive N-methyl-D-aspartate (NMDA) receptor antagonists, LY274614, LY233536 and LY235723, on the micturition reflex and external urethral sphincter EMG activity, were examined either under isovolumetric conditions or during continuous filling cystometry in urethane-anaesthetized (1.2 g kg-1, s...

journal_title：British journal of pharmacology

authors： Yoshiyama M,Roppolo JR,Thor KB,de Groat WC

更新日期：1993-09-01 00:00:00

abstract：:The extracellular matrix (ECM) is a salient feature of all solid tissues within the body. This complex, acellular entity is composed of hundreds of individual molecules whose assembly, architecture and biomechanical properties are critical to controlling the behaviour and phenotype of the different cell types residing...

journal_title：British journal of pharmacology

authors： Hastings JF,Skhinas JN,Fey D,Croucher DR,Cox TR

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Substance P (SP) and calcitonin gene-related peptide (CGRP) released from capsaicin-sensitive sensory nerves induce local neurogenic inflammation; somatostatin exerts systemic anti-inflammatory actions presumably via sst4/sst1 receptors. This study investigates the effects of a high affinity, sst...

journal_title：British journal of pharmacology

authors： Helyes Z,Pintér E,Németh J,Sándor K,Elekes K,Szabó A,Pozsgai G,Keszthelyi D,Kereskai L,Engström M,Wurster S,Szolcsányi J

更新日期：2006-10-01 00:00:00

abstract：:1. Using a guinea-pig model of allergic asthma, in which the animals display early (0-5 h) and late phase (8-23 h after antigen challenge) bronchoconstrictor reactions, the function of prejunctional inhibitory M2 and postjunctional M3 receptors in isolated tracheal preparations have been investigated. In addition, car...

journal_title：British journal of pharmacology

authors： ten Berge RE,Santing RE,Hamstra JJ,Roffel AF,Zaagsma J

更新日期：1995-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Transient receptor potential melastatin 3 (TRPM3) proteins form non-selective but calcium-permeable membrane channels, rapidly activated by extracellular application of the steroid pregnenolone sulphate and the dihydropyridine nifedipine. Our aim was to characterize the steroid binding site by an...

journal_title：British journal of pharmacology

authors： Drews A,Mohr F,Rizun O,Wagner TF,Dembla S,Rudolph S,Lambert S,Konrad M,Philipp SE,Behrendt M,Marchais-Oberwinkler S,Covey DF,Oberwinkler J

更新日期：2014-02-01 00:00:00

abstract：:1. By use of patch-clamp techniques, the effects of SD-3212, a novel antiarrhythmic drug, on the calcium current (Ica), the sodium current (INa) and the muscarinic acetylcholine-receptor-operated potassium current (IK.ACh) were examined and compared with those of bepridil in guinea-pig single atrial cells. 2. SD-3212 ...

journal_title：British journal of pharmacology

authors： Hara Y,Nakaya H

更新日期：1995-11-01 00:00:00

abstract：:1. In urethane-anaesthetized guinea-pigs, under spontaneous respiration, indomethacin (1 mg kg-1 i.v., 10-45 min) approximately doubled the bronchoconstrictor effect (increase in airways resistance, R(aw)) of equieffective doses of histamine and 5-hydroxytryptamine (5-HT), but not that of acetylcholine or leukotriene ...

journal_title：British journal of pharmacology

authors： Mitchell HW,Adcock J

更新日期：1988-06-01 00:00:00

abstract：:1. We aimed to determine whether nitric oxide (NO) and/or the endothelium is involved in cholinergic neurogenic vasodilatation in the rat isolated hindquarters. 2. The abdominal aorta was cannulated for perfusion of the rat hindquarters with Krebs bicarbonate solution containing phenylephrine, to induce basal constric...

journal_title：British journal of pharmacology

authors： Loke KE,Sobey CG,Dusting GJ,Woodman OL

更新日期：1994-06-01 00:00:00

abstract：:1. The mechanisms involved in tachykinin-induced oedema were investigated in rat skin and interactions between the tachykinins and calcitonin gene-related peptide (CGRP) were studied. 2. Intradermal injections of the tachykinins, substance P, neurokinin A and neurokinin B, stimulated local oedema formation which was i...

journal_title：British journal of pharmacology

authors： Brain SD,Williams TJ

更新日期：1989-05-01 00:00:00

abstract：:Mitochondrial permeability transition pore (mPTP) opening plays a critical role in cardiac reperfusion injury and its prevention is cardioprotective. Tumour cell mitochondria usually have high levels of hexokinase isoform 2 (HK2) bound to their outer mitochondrial membranes (OMM) and HK2 binding to heart mitochondria ...

journal_title：British journal of pharmacology

authors： Halestrap AP,Pereira GC,Pasdois P

更新日期：2015-04-01 00:00:00

abstract：:The sensitivity of the uterus to the inhibition of contractions by salbutamol, diltiazem or nifedipine was assessed in the ovariectomized, post-partum rat by dose-response curves following bolus intravenous (i.v.) administration. These tests were performed before (day 1), immediately after a 20 h i.v. infusion of salb...

journal_title：British journal of pharmacology

authors： Abel MH,Hollingsworth M

更新日期：1986-07-01 00:00:00

abstract：:1. Endothelin-1 (ET-1) binding site densities and constrictor activities were compared in airway smooth muscle preparations of human, guinea-pig, rat and mouse. 2. The mean contractile response to 0.3 microM ET-1 (measured as the % maximum response to 10 microM carbachol, % Cmax +/- s.e.mean) and the mean concentratio...

journal_title：British journal of pharmacology

authors： Henry PJ,Rigby PJ,Self GJ,Preuss JM,Goldie RG

更新日期：1990-08-01 00:00:00

abstract：:Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs). Agonist affinity may be estimated in terms of the dissociation const...

journal_title：British journal of pharmacology

authors： Strange PG

更新日期：2008-04-01 00:00:00

abstract：:1 Both phasic and tonic responses to KCl 160 mM were reduced by Ca2+ deprivation. After 90 min, the phasic response was abolished but 13 +/- 1.5% of the tonic response remained. This resistant component was still present if the Ca2+-free solution contained EGTA 0.1 mM. The tonic response was more resistant to deprivat...

journal_title：British journal of pharmacology

authors： Hay DW,Wadsworth RM

更新日期：1982-05-01 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：:1. The role of sodium-calcium exchanger in acetylcholine (Ach)-induced hyperpolarization of intact endothelial cells was studied in excised rat aorta. The membrane potential was recorded using perforated patch-clamp technique. 2. The mean resting potential of endothelial cells was -44.1+/-1.4 mV. A selective inhibitor...

journal_title：British journal of pharmacology

authors： Bondarenko A

更新日期：2004-09-01 00:00:00

abstract：:We have examined whether modulation of the polyamine biosynthetic pathway, through inhibition by alpha-difluoromethylornithine (DFMO) of the rate limiting enzyme, ornithine decarboxylase (ODC), modulates NO synthesis in J774 macrophages. DFMO potentiated LPS-stimulated nitrite production in both a concentration- and t...

journal_title：British journal of pharmacology

authors： Baydoun AR,Morgan DM

更新日期：1998-12-01 00:00:00

abstract：:1. The actions on the taenia of 4-(m-chlorophenylcarbamoyloxy)-2-butynyl-trimethylammonium chloride (McN-A-343), N-benzyl-3-pyrrolidyl acetate methobromide (AHR-602), tetramethylammonium (TMA) and choline phenyl ether have been examined and compared with the actions of acetylcholine, nicotine and 1,1-dimethyl-4-phenyl...

journal_title：British journal of pharmacology

authors： Hobbiger F,Mitchelson F,Rand MJ

更新日期：1969-05-01 00:00:00

abstract：:Strips of human pulmonary arteries from patients undergoing surgery for lung tumour were incubated with [3H]-noradrenaline. Subsequently, they were superfused with physiological salt solution containing cocaine and corticosterone. Tritium overflow from the strips was stimulated by transmural electrical impulses (2 Hz)...

journal_title：British journal of pharmacology

authors： Göthert M,Hentrich F

更新日期：1985-08-01 00:00:00

abstract：:Platelet-activating factor (Paf) has been proposed as a mediator of the gastrointestinal damage in endotoxic shock. The formation of Paf in rat jejunal tissue, determined following extraction and bioassay on rabbit washed platelets has therefore been correlated with the induction of damage following endotoxin administ...

journal_title：British journal of pharmacology

authors： Whittle BJ,Boughton-Smith NK,Hutcheson IR,Esplugues JV,Wallace JL

更新日期：1987-09-01 00:00:00

abstract：:Adenosine 5'-diphosphate (ADP) induces human platelet aggregation and inhibits stimulated adenylate cyclase. Adenosine 5'-O-(1-thiodiphosphate) (ADP-alpha-S) and adenosine 5'-O-(2-thiodiphosphate) (ADP-beta-S) act at the ADP receptor and achieve the same maximal rate of human platelet aggregation as each other. Adenos...

journal_title：British journal of pharmacology

authors： Cusack NJ,Hourani SM

更新日期：1982-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The chemokine receptor CXCR3 directs migration of T-cells in response to the ligands CXCL9/Mig, CXCL10/IP-10 and CXCL11/I-TAC. Both ligands and receptors are implicated in the pathogenesis of inflammatory disorders, including atherosclerosis and rheumatoid arthritis. Here, we describe the molecul...

journal_title：British journal of pharmacology

authors： Nedjai B,Li H,Stroke IL,Wise EL,Webb ML,Merritt JR,Henderson I,Klon AE,Cole AG,Horuk R,Vaidehi N,Pease JE

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hypoxia/reoxygenation induces synthesis of reactive oxygen species (ROS) which can attack macromolecules and cause brain injury. The transcription factor, nuclear factor (erythroid-derived 2)-like 2, (Nrf2), ia potent activator of genes with an antioxidant responsive element and Nrf2 can countera...

journal_title：British journal of pharmacology

authors： Cao S,Chao D,Zhou H,Balboni G,Xia Y

更新日期：2015-04-01 00:00:00