Effect of the hypoglycaemic drug (-)-AZ-DF-265 on ATP-sensitive potassium channels in rat pancreatic beta-cells.

abstract：:1. Rabbit isolated irides were loaded with [3H]-noradrenaline and superfused with Tyrode solution. The inhibition by the muscarinic agonists (+/-)-methacholine and pilocarpine of the [3H]-noradrenaline overflow into the superfusate evoked by field stimulation (pulses of 1 ms duration, 75 mA) was measured as an index o...

journal_title：British journal of pharmacology

authors： Bognar IT,Pallas S,Fuder H,Muscholl E

更新日期：1988-07-01 00:00:00

abstract：:1. SCA40 (1nM-10 microM), isoprenaline (1-300 nM) and levcromakalim (100 nM-10 microM) each produced concentration-dependent suppression of the spontaneous tone of guinea-pig isolated trachea. Propranolol (1 microM) markedly (approximately 150 fold) antagonized isoprenaline but did not antagonize SCA40. The tracheal r...

journal_title：British journal of pharmacology

authors： Cook SJ,Archer K,Martin A,Buchheit KH,Fozard JR,Müller T,Miller AJ,Elliott KR,Foster RW,Small RC

更新日期：1995-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:While the 5-HT and Rho-kinase (ROCK) pathways have been implicated in the development of pulmonary arterial hypertension (PAH), the nature of any interactions between them remain unclear. This study investigated a role for ROCK in 5-HT-regulated proliferative responses in lung fibroblasts in vivo...

journal_title：British journal of pharmacology

authors： Mair KM,MacLean MR,Morecroft I,Dempsie Y,Palmer TM

更新日期：2008-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Normal pregnancy is associated with decreased vascular resistance and increased release of vasodilators. Endothelin-1 (ET-1) causes vasoconstriction via endothelin receptor type A (ET(A)R), but could activate ET(B)R in the endothelium and release vasodilator substances. However, the roles of ET(B...

journal_title：British journal of pharmacology

authors： Mazzuca MQ,Dang Y,Khalil RA

更新日期：2013-07-01 00:00:00

abstract：:1 Weighed stripped vasa deferentia were incubated in Holman's solution containing (a) [14C]-sorbitol 0.014 mm, (b) [3H]-noradrenaline ([3H]-NA) 12.31 nM, (c) [3H]-tetrahydrocannabinol ([3H]-delta1-THC) 1 mug/ml for 5, 10, 20 and 30 minutes. 2 Tissues were washed, dissolved in Protosol, counted by standard scintillatio...

journal_title：British journal of pharmacology

authors： Egan SM,Graham JD,Lewis MJ

更新日期：1976-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Kinins are pro-inflammatory peptides that are released during tissue injury, including that caused by inflammatory bowel disease. Herein, we assessed the role and underlying mechanisms through which the absence of kinin B(1) receptors exacerbates the development of dextran sulfate sodium (DSS)-i...

journal_title：British journal of pharmacology

authors： Marcon R,Claudino RF,Dutra RC,Bento AF,Schmidt EC,Bouzon ZL,Sordi R,Morais RL,Pesquero JB,Calixto JB

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Mast cells are important in allergic reactions. Here, we assessed the anti-allergic effects of the anti-cancer drug tozasertib specifically regarding regulatory effects on mast cell activation. EXPERIMENTAL APPROACH:Tozasertib effects on mast cell degranulation were determined by measuring β-hex...

journal_title：British journal of pharmacology

authors： Zhang LN,Ji K,Sun YT,Hou YB,Chen JJ

更新日期：2020-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GoSlo-SR compounds are efficacious BK (KCa 1.1) channel openers, but little is known about their mechanism of action or effect on bladder contractility. We examined the effects of two closely related compounds on BK currents and bladder contractions. EXPERIMENTAL APPROACH:A combination of electr...

journal_title：British journal of pharmacology

authors： Large RJ,Kshatri A,Webb TI,Roy S,Akande A,Bradley E,Sergeant GP,Thornbury KD,McHale NG,Hollywood MA

更新日期：2015-05-01 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：:1. Male, Long Evans rats were instrumented chronically with pulsed Doppler probes and intravascular catheters to allow assessment of regional haemodynamic changes during i.v. infusion of lipopolysaccharide (LPS, 150 micrograms kg-1 h-1). 2. In the presence of the AT1-receptor antagonists, losartan (10 mg kg-1 + 10 kg-...

journal_title：British journal of pharmacology

authors： Gardiner SM,Kemp PA,March JE,Bennett T

更新日期：1996-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-arachidonyl dopamine (NADA) has been identified as a putative endocannabinoid, but there is little information about which signalling pathways it activates. The purpose of this study was to identify the signalling pathways activated by NADA in vitro. EXPERIMENTAL APPROACH:Human or rat cannabin...

journal_title：British journal of pharmacology

authors： Redmond WJ,Cawston EE,Grimsey NL,Stuart J,Edington AR,Glass M,Connor M

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-invasive in vivo imaging of cannabinoid CB2 receptors using PET is pursued to study neuroinflammation. The purpose of this study is to evaluate the in vivo binding specificity of [18 F]MA3, a CB2 receptor agonist, in a rat model with local overexpression of human (h) CB2 receptors. METHODS:[...

journal_title：British journal of pharmacology

authors： Attili B,Celen S,Ahamed M,Koole M,Haute CVD,Vanduffel W,Bormans G

更新日期：2019-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Our team previously demonstrated that diabetes induces a deterioration in vascular dynamics, in parallel with the enhanced formation of advanced glycation end products. The aim of this study was to determine whether prevention of the arterial stiffening by pyridoxamine in diabetes is associated w...

journal_title：British journal of pharmacology

authors： Chang KC,Liang JT,Tsai PS,Wu MS,Hsu KL

更新日期：2009-08-01 00:00:00

abstract：:1. The prostate function is regulated by androgens and alpha-adrenergic activity. Clinically, antiandrogens and/or alpha(1)-adrenergic antagonists are commonly used to treat symptomatic prostatic hypertrophy. To elucidate the effects of androgen deprivation on prostate contractility via alpha(1)-adrenoceptor, the char...

journal_title：British journal of pharmacology

authors： Homma Y,Hamada K,Nakayama Y,Tsujimoto G,Kawabe K

更新日期：2000-12-01 00:00:00

abstract：:1. The mechanism underlying the anticataleptic properties of the atypical neuroleptic agent, clozapine, has been investigated in the rat. 2.The close structural analogues of clozapine, loxapine (0.1 mg kg(-1) s.c.) and iso-clozapine (1 and 3 mg kg(-1) s.c.) induced catalepsy in rats. In contrast, clozapine and the reg...

journal_title：British journal of pharmacology

authors： Kalkman HO,Neumann V,Hoyer D,Tricklebank MD

更新日期：1998-08-01 00:00:00

abstract：:1. DL-1-(2-acetyl-4-n-butyramidophenoxy)-2-hydroxy-3-isopropylaminopropane hydrochloride (M & B 17803A) was given to four healthy volunteers in single oral doses of up to 300 mg. There were no subjective effects and no significant alterations in the heart rate, systolic and diastolic blood pressure in the seated posit...

journal_title：British journal of pharmacology

authors： Cuthbert MF,Owusu-Ankomah K

更新日期：1971-11-01 00:00:00

abstract：:1. The actions of bretylium tosylate on neuromuscular transmission in the rat phrenic nerve diaphragm preparation have been investigated by electro-2. On the guinea-pig ileum, threshold doses elicit repeated maximal spike contractions which are blocked by atropine. In the presence of atropine, higher concentrations of...

journal_title：British journal of pharmacology

authors： Clineschmidt BV,Geller RG,Govier WC,Pisano JJ,Tanimura T

更新日期：1971-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aim of this study was to determine whether the apelin/APJ system is altered in human cardiovascular disease by investigating whether the expression of apelin or its receptor is altered at the protein level. EXPERIMENTAL APPROACH:Radioligand binding studies were used to determine apelin recep...

journal_title：British journal of pharmacology

authors： Pitkin SL,Maguire JJ,Kuc RE,Davenport AP

更新日期：2010-08-01 00:00:00

abstract：:1. We studied the stereoselectivity of the effects of the enantiomers of the cardiotonic agent DPI 201-106 (4-[3'-(4"-benzhydryl-1"-piperazinyl)-2'-hydroxypropoxy]-1H-indole-2- carbonitrile, DPI) and its methyl-for-carbonitrile analogue BDF 8784 on cardiac calcium currents (ICa) of guinea-pig ventricular myocytes. The...

journal_title：British journal of pharmacology

authors： Ravens U,Pfeifer T,Wettwer E,Grundke M

更新日期：1991-10-01 00:00:00

abstract：:Among the five human 5-HT(4) (h5-HT(4)) receptor isoforms, the h5-HT(4(a)) receptor was studied with a particular emphasis on the molecular interactions involved in ligand binding. For this purpose, we used site-directed mutagenesis of the transmembrane domain. Twelve mutants were constructed with a special focus on t...

journal_title：British journal of pharmacology

authors： Mialet J,Dahmoune Y,Lezoualc'h F,Berque-Bestel I,Eftekhari P,Hoebeke J,Sicsic S,Langlois M,Fischmeister R

更新日期：2000-06-01 00:00:00

abstract：:1 The L6 myocyte cell line expresses high affinity receptors for calcitonin gene-related peptide (CGRP) which are coupled to activation of adenylyl cyclase. The biochemical pharmacology of these receptors has been examined by radioligand binding or adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation. 2 In i...

journal_title：British journal of pharmacology

authors： Poyner DR,Andrew DP,Brown D,Bose C,Hanley MR

更新日期：1992-02-01 00:00:00

abstract：:1. The purpose of the present study was to determine the myocardial cytoprotective efficacy of azapropazone (AZA) and its potential site of action on neutrophil infiltration into reperfused/ischaemic myocardium with or without in vivo activation of neutrophils in rabbits. 2. AZA, 100 mg kg-1, was administered i.v. 10 ...

journal_title：British journal of pharmacology

authors： Mousa SA,Brown R,Thoolen MJ,Smith RD

更新日期：1990-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The human kinome consists of roughly 500 kinases, including 150 that have been proposed as therapeutic targets. Protein kinases regulate an array of signalling pathways that control metabolism, cell cycle progression, cell death, differentiation and survival. It is not surprising, then, that new ...

journal_title：British journal of pharmacology

authors： Jensen BC,Parry TL,Huang W,Beak JY,Ilaiwy A,Bain JR,Newgard CB,Muehlbauer MJ,Patterson C,Johnson GL,Willis MS

更新日期：2017-12-01 00:00:00

abstract：:1. Microfluorimetry techniques with fura-2 were used to characterize the effects of efaroxan (200 microM), phenotolamine (200-500 microM) and idazoxan (200-500 microM) on the intracellular free Ca2+ concentration ([Ca2+]i) in mouse isolated islets of Langerhans. 2. The imidazoline receptor agonists efaroxan and phento...

journal_title：British journal of pharmacology

authors： Shepherd RM,Hashmi MN,Kane C,Squires PE,Dunne MJ

更新日期：1996-11-01 00:00:00

abstract：:1 About 45% of singly-housed male mice showed timidity (alert postures, running away, defensive postures) instead of aggression on interactions in pairs with group-housed male mice, though their partners did not show any aggression. The isolation-induced timidity was stable in repeated interactions. Timid mice also sh...

journal_title：British journal of pharmacology

authors： Krsiak M

更新日期：1975-09-01 00:00:00

abstract：:1. The present study shows the effects of imipramine in a single dose (10 mg kg(-1), p.o.) or following repeated (14 days, twice a day) treatment on the level of mRNA coding for D2 dopamine receptors in the rat caudate putamen (CP). Repeated administration of imipramine resulted in the increase of the level of mRNA co...

journal_title：British journal of pharmacology

authors： Dziedzicka-Wasylewska M,Rogoz R

更新日期：1998-03-01 00:00:00

abstract：:1. The mechanisms by which nicorandil causes relaxation of rat isolated small mesenteric arteries mounted on a Mulvany myograph was investigated by use of a combination of putatively mechanism-specific antagonists. 2. In arteries precontracted by the thromboxane-mimetic, U46619, the EC50 for cromakalim and levcromakal...

journal_title：British journal of pharmacology

authors： Fujiwara T,Angus JA

更新日期：1996-12-01 00:00:00

abstract：:1. Inhibition of rat platelet aggregation by the nitric oxide (NO) donor MAHMA NONOate (Z-1-N-methyl-N-[6-(N-methylammoniohexyl)amino]diazen-1-ium-1,2-diolate) was investigated. The aims were to compare its anti-aggregatory effect with vasorelaxation, to determine the effects of the soluble guanylate cyclase inhibitor...

journal_title：British journal of pharmacology

authors： Homer KL,Wanstall JC

更新日期：2002-12-01 00:00:00

abstract：:1. The action of angiotensin on the circular and longitudinal muscle of the human colon has been studied in vitro. The ED50 value (g/ml) of circular muscle was 8.7 x 10(-8) and of longitudinal muscle 3.1 x 10(-8), while the corresponding figures for acetylcholine were 1.6 x 10(-6) and 1.1 x 10(-6), respectively. Angio...

journal_title：British journal of pharmacology

authors： Fishlock DJ,Gunn A

更新日期：1970-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:(R,S)-ketamine produces rapid and significant antidepressant effects in approximately 65% of patients suffering from treatment-resistant bipolar depression (BD). The genetic, pharmacological and biochemical differences between ketamine responders and non-responders have not been identified. The p...

journal_title：British journal of pharmacology

authors： Villaseñor A,Ramamoorthy A,Silva dos Santos M,Lorenzo MP,Laje G,Zarate C Jr,Barbas C,Wainer IW

更新日期：2014-04-01 00:00:00