[(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors.

abstract：BACKGROUND AND PURPOSE:Small molecule glucokinase activators (GKAs) have been associated with potent antidiabetic efficacy and hepatic steatosis in rodents. This study reports the discovery of S 50131 and S 51434, two novel GKAs with an original scaffold and an atypical pharmacological profile. EXPERIMENTAL APPROACH:A...

journal_title：British journal of pharmacology

authors： De Ceuninck F,Kargar C,Charton Y,Goldstein S,Perron-Sierra F,Ilic C,Caliez A,Rolin JO,Sadlo M,Harley E,Vinson C,Ktorza A

更新日期：2013-07-01 00:00:00

abstract：:1. The effects of intracameral injections of prostaglandins E(1), E(2), F(1a), F(2a), and A(1) were studied on the intraocular pressure (IOP) of rabbits anaesthetized with urethane.2. With the exception of prostaglandin F(1a), all the prostaglandins studied were found to be capable of producing a large, sustained rise...

journal_title：British journal of pharmacology

authors： Beitch BR,Eakins KE

更新日期：1969-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The chemokine receptor CXCR3 is implicated in a variety of clinically important diseases, notably rheumatoid arthritis and atherosclerosis. Consequently, antagonists of CXCR3 are of therapeutic interest. In this study, we set out to characterize binding sites of the specific low MW CXCR3 antagoni...

journal_title：British journal of pharmacology

authors： Nedjai B,Viney JM,Li H,Hull C,Anderson CA,Horie T,Horuk R,Vaidehi N,Pease JE

更新日期：2015-04-01 00:00:00

abstract：:1. In the presence of atropine, mepyramine and ranitidine, electric field stimulation of the guinea-pig isolated ileum longitudinal muscle-myenteric plexus preparation resulted in a two component non-adrenergic non-cholinergic contraction. The initial contraction had a duration of approximately 1 s whereas the second ...

journal_title：British journal of pharmacology

authors： Taylor SJ,Kilpatrick GJ

更新日期：1992-03-01 00:00:00

abstract：:1. This study investigates the effect of partially metabolic controlled long-term (34 weeks) streptozotocin (STZ)-induced diabetes on relaxation and contractile responses of isolated coronary arteries to seven different vasoactive agents. 2. The average fasting and non-fasting blood glucose concentrations (mM) were si...

journal_title：British journal of pharmacology

authors： Sheykhzade M,Dalsgaard GT,Johansen T,Nyborg NC

更新日期：2000-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Selective oestrogen receptor (ER) modulators (SERMs) are of great value in the treatment of breast cancer and osteoporosis. The aim of this study was to characterize pharmacologically a new class of SERMs synthesized based on the core structure of raloxifene. EXPERIMENTAL APPROACH:Competitive re...

journal_title：British journal of pharmacology

authors： Ning M,Zhou C,Weng J,Zhang S,Chen D,Yang C,Wang H,Ren J,Zhou L,Jin C,Wang MW

更新日期：2007-01-01 00:00:00

abstract：:1--Responses (relaxation) to the beta-adrenoceptor agonists, isoprenaline, fenoterol or noradrenaline, were obtained on cat tracheal preparations contracted with a submaximal concentration of carbachol (0.5 microM). 2--The relative potencies of isoprenaline: fenoterol: noradrenaline were 100:8.1:10.7. From this, it wa...

journal_title：British journal of pharmacology

authors： O'Donnell SR,Wanstall JC

更新日期：1983-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cloxyquin (5-cloroquinolin-8-ol) has been described as an activator of TRESK (K2P 18.1, TWIK-related spinal cord K+ channel) background potassium channel. We have examined the specificity of the drug by testing several K2P channels. We have investigated the mechanism of cloxyquin-mediated TRESK a...

journal_title：British journal of pharmacology

authors： Lengyel M,Dobolyi A,Czirják G,Enyedi P

更新日期：2017-07-01 00:00:00

abstract：:1. Magnesium sulphate was studied for its effects on diarrhoea, fluid secretion, gastrointestinal transit and nitric oxide (NO) synthase activity in rats. 2. At a dose of 2 g kg-1 orally magnesium sulphate produced diarrhoea that was delayed in onset and intensity in a dose-related manner by the NO synthase inhibitor ...

journal_title：British journal of pharmacology

authors： Izzo AA,Gaginella TS,Mascolo N,Capasso F

更新日期：1994-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The endocannabinoid system and the cannabinoid CB(1) receptor have been identified in human sperm, and it is well known that endocannabinoids have pronounced adverse effects on male and female reproduction. In order to elucidate further the pathophysiological role of the endocannabinoid system in...

journal_title：British journal of pharmacology

authors： Aquila S,Guido C,Santoro A,Gazzerro P,Laezza C,Baffa MF,Andò S,Bifulco M

更新日期：2010-02-01 00:00:00

abstract：:Effects of isoprenaline (Isop) on the contractile properties of the smooth muscle cells of cat trachea were investigated using intact and chemically skinned muscle preparations and an isometric tension recording method. In the intact muscle preparations, Isop 3 X 10(-10) or 3 X 10(-9) M significantly suppressed the am...

journal_title：British journal of pharmacology

authors： Ito Y,Itoh T

更新日期：1984-11-01 00:00:00

abstract：:1. The aim of the study was to investigate the mechanism of a novel effect of hypoxia on intracellular Ca(2+) signalling in rabbit cerebral arteriolar smooth muscle cells, an effect that was resistant to the L-type Ca(2+) channel antagonist methoxyverapamil (D600). 2.[Ca(2+)](i) of smooth muscle cells in intact arteri...

journal_title：British journal of pharmacology

authors： Guibert C,Flemming R,Beech DJ

更新日期：2002-02-01 00:00:00

abstract：:Authentic nitric oxide (NO; 0.1 - 10 micromoles) caused transient, dose-dependent relaxation of phenylephrine-induced tone without changing membrane potential in mesenteric arteries. Larger doses, above 10 micromoles, did not evoke more relaxation (maximal relaxation to 150 micromoles NO in denuded arteries, 69+/-7%, ...

journal_title：British journal of pharmacology

authors： Plane F,Sampson LJ,Smith JJ,Garland CJ

更新日期：2001-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In patients with pulmonary hypertension (PH) associated with lung disease and/or hypoxia (Group III), decreased pulmonary vascular tone and tissue hypoxia is therapeutically beneficial. PGE2 and PGI2 induce potent relaxation of human bronchi from non-PH (control) patients via EP4 and IP receptors...

journal_title：British journal of pharmacology

authors： Ozen G,Benyahia C,Mani S,Boukais K,Silverstein AM,Bayles R,Nelsen AC,Castier Y,Danel C,Mal H,Clapp LH,Longrois D,Norel X

更新日期：2020-01-01 00:00:00

abstract：:1. Prostaglandins and the vasodilator neuropeptide, calcitonin-gene related peptide (CGRP), have both been implicated in the pathogenesis of migraine headache. We have used primary cultures of adult rat trigeminal neurones to examine the effects of prostanoids on CGRP release in vitro. 2. CGRP release was stimulated b...

journal_title：British journal of pharmacology

authors： Jenkins DW,Feniuk W,Humphrey PP

更新日期：2001-11-01 00:00:00

abstract：:The vasorelaxant activity of eicosapentaenoic acid (EPA, 20:5n-3), the omega-3 polyunsaturated fatty acid, was investigated in isolated Wistar Kyoto (WKY) rat aortae by measuring isometric tension. Eicosapentaenoic acid (1 - 100 microM) relaxed rat aortae contracted with high K(+) (80 mM) or noradrenaline (NA, 1 micro...

journal_title：British journal of pharmacology

authors： Engler MB,Engler MM,Browne A,Sun YP,Sievers R

更新日期：2000-12-01 00:00:00

abstract：:1. Hypercholesterolaemia often occurs in patients with type 2 diabetes, who therefore encounter administration of HMG-CoA reductase inhibitors. Alteration of pancreatic beta-cell function leading to an impaired insulin secretory response to glucose plays a crucial role in the pathogenesis of type 2 diabetes. Therefore...

journal_title：British journal of pharmacology

authors： Yada T,Nakata M,Shiraishi T,Kakei M

更新日期：1999-03-01 00:00:00

abstract：:delta 9-Tetrahydrocannabinol (delta 9-THC) was injected into the preoptic area of the anterior hypothalamus or into the third or fourth cerebral ventricle of the conscious mouse through a chronically implanted cannula and the effects on body temperature and oxygen consumption rate were measured. At an ambient temperat...

journal_title：British journal of pharmacology

authors： Fitton AG,Pertwee RG

更新日期：1982-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Central anti-nociceptive actions of baclofen involve activation of K+ channels. Here we assessed what types of K+ channel might participate in the peripheral anti-nociception induced by baclofen. EXPERIMENTAL APPROACH:Nociceptive thresholds to mechanical stimulation in rat paws treated with intr...

journal_title：British journal of pharmacology

authors： Reis GM,Duarte ID

更新日期：2006-11-01 00:00:00

abstract：:1. Therapeutic doses of colistin sulphomethate sodium B.P. (Colomycin), pento-N sulphomethylpolymyxin B sodium (Thiosporin) and ampicillin B.P. (Penbritin) as well as normal saline have been given to volunteers with normal kidney function.2. A blind crossover technique was used and the effects of the compounds on bloo...

journal_title：British journal of pharmacology

authors： Caldwell AD,Martin AJ,Trigger DJ

更新日期：1969-09-01 00:00:00

abstract：:1. The expression of hepatocyte growth factor (HGF) is essential for normal placental development although its function is unknown. In this study we examined the effect of HGF on trophoblast cell motility and invasion of fibrin gels and investigated the possible role of nitric oxide (NO) in this process. 2. The human ...

journal_title：British journal of pharmacology

authors： Cartwright JE,Holden DP,Whitley GS

更新日期：1999-09-01 00:00:00

abstract：:1. Alprenolol, a beta-adrenoceptor blocking drug reported to have the same potency as propranolol in vitro and in vivo, was found to be four times more active than procaine as a local anaesthetic on frog sciatic nerve.2. At doses of 0.125 mg/kg and above alprenolol protected anaesthetized guinea-pigs against ouabain-i...

journal_title：British journal of pharmacology

authors： Singh BN,Williams EM

更新日期：1970-04-01 00:00:00

abstract：:1. Acute moderate hypoxia modifies the catalytic activity and expression of certain isoenzymes of hepatic cytochrome P450 (P450). The aim of this study was to document whether hypoxia affects hepatic P450 directly or through the release of serum mediators. 2. Rabbits were subjected to a FiO(2) of 8% for 48 h, sacrific...

journal_title：British journal of pharmacology

authors： Fradette C,Bleau AM,Pichette V,Chauret N,Du Souich P

更新日期：2002-11-01 00:00:00

abstract：:Forty-eight isolated rat hearts were perfused with Krebs solution and with [(3)H]-(-)-noradrenaline ([(3)H]-NA) containing 4.5 nCi/ml in 50 ng/ml, as described by Iversen (1963). To groups of six, cocaine was added to [(3)H]-NA in concentrations of 400 nM, 2 and 10 muM. To the rest Tween 80, 25 mug/ml was added to [(3...

journal_title：British journal of pharmacology

authors： Graham JD,Lewis MJ,Li DM

更新日期：1974-07-01 00:00:00

abstract：:1. Various neurotransmitters in the brain regulate gastric acid secretion. Previously, we reported that the central injection of kappa-opioid receptor agonists stimulated this secretion in rats. Although the existence of kappa(1)-kappa(3)-opioid receptor subtypes has been proposed, the character is not defined. We inv...

journal_title：British journal of pharmacology

authors： Minowa S,Ishihara S,Tsuchiya S,Horie S,Watanabe K,Murayama T

更新日期：2003-03-01 00:00:00

abstract：:1 New 2H-1,4-benzoxazine derivatives were synthesized and tested for their agonist properties on the ATP-sensitive K(+) channels (K(ATP)) of native rat skeletal muscle fibres by using the patch-clamp technique. The novel modifications involved the introduction at position 2 of the benzoxazine ring of alkyl substituent...

journal_title：British journal of pharmacology

authors： Tricarico D,Barbieri M,Antonio L,Tortorella P,Loiodice F,Camerino DC

更新日期：2003-05-01 00:00:00

abstract：:Muscarinic receptors in the rat cerebral cortex, reacted with p-chloromercuribenzoate (PCMB) under different conditions (Phase I and II), have modified binding sites. These exhibit remarkable changes in the structural dependence of the binding of drugs. In Phase I, the structure-binding profile of agonists for both th...

journal_title：British journal of pharmacology

authors： Birdsall NJ,Burgen AS,Hulme EC,Wong EH

更新日期：1983-09-01 00:00:00

abstract：:1. The regional binding of [3H]-(+)-5-methyl-10,11-dihydro-5H-dibenzo (a,d)cyclohepten-5,10-imine maleate ([3H]-(+)-MK 801) to sections of rat brain was measured by an in vitro quantitative autoradiographic technique. A heterogeneous distribution of binding sites was observed. 2. High values of binding were detected i...

journal_title：British journal of pharmacology

authors： Tacconi S,Ratti E,Marien MR,Gaviraghi G,Bowery NG

更新日期：1993-03-01 00:00:00

abstract：:1. The ratio of the content of vasopressin to that of oxytocin (V/O ratio) was estimated in the supraoptic nucleus (SON), paraventricular nucleus (PVN) and posterior pituitary gland (PIT) of guinea-pigs.2. Extracts were assayed for antidiuretic activity to estimate vasopressin and for milk-ejecting activity to estimat...

journal_title：British journal of pharmacology

authors： Bisset GW,Errington ML,Richards CD

更新日期：1973-06-01 00:00:00

abstract：:1 The venom of the green mamba, Dendroaspis angusticeps, was tested for effects on neuromuscular transmission and skeletal muscle contractility in isolated phrenic nerve-hemidiaphragm preparations of the rat and mouse, chick biventer cervicis muscle preparations and in aneural cultures of embryonic chick skeletal musc...

journal_title：British journal of pharmacology

authors： Barrett JC,Harvey AL

更新日期：1979-10-01 00:00:00