Glimepiride block of cloned beta-cell, cardiac and smooth muscle K(ATP) channels.

abstract：:1. Adenosine 5'-triphosphate (ATP) is known to augment cardiac contractile activity and cause an increase in intracellular Ca(2+) concentration ([Ca(2+)](i)) in isolated cardiomyocytes. However, no information regarding the ATP-mediated signal transduction in the myocardium in congestive heart failure (CHF) is availab...

journal_title：British journal of pharmacology

authors： Saini HK,Shao Q,Musat S,Takeda N,Tappia PS,Dhalla NS

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Heparin is known to possess a range of activities, other than effects on blood coagulation, many of which are anti-inflammatory. Effects with potential anti-inflammatory applications include the inhibition of elastase release from neutrophils, as well as the adhesion of these cells to vascular en...

journal_title：British journal of pharmacology

authors： Lever R,Lo WT,Faraidoun M,Amin V,Brown RA,Gallagher J,Page CP

更新日期：2007-07-01 00:00:00

abstract：:1 The effect of phenoxybenzamine on the efflux of [3H]-noradrenaline and the mechanical response to single pulse excitation of superfused guinea-pig vas deferens was determined to examine the validity of the currently accepted hypothesis of a presynaptic negative feedback system on adrenergic nerve terminals. 2 The ad...

journal_title：British journal of pharmacology

authors： Kalsner S

更新日期：1979-06-01 00:00:00

abstract：:1. The noradrenaline (NA) concentration in the "heart" (atria and right ventricle) of male rats was estimated at different periods following adrenal demedullation. For 1-3 weeks after the operation there was, in all rats, a reduction in NA content of the tissue, whereas, after somewhat longer intervals, the concentrat...

journal_title：British journal of pharmacology

authors： Borchard F,Vogt M

更新日期：1970-01-01 00:00:00

abstract：:1. Muscarinic receptors present in the human astrocytoma cell line 1321 N1 were characterized in radioligand binding studies and in functional studies of carbachol-stimulated phosphatidylinositol (PI) turnover. 2. In radioligand binding studies the muscarinic receptor in intact cells could be labelled using [3H]-N-met...

journal_title：British journal of pharmacology

authors： Kunysz EA,Michel AD,Whiting RL,Woods K

更新日期：1989-02-01 00:00:00

abstract：:1. The putative alpha 1-adrenoceptor subtypes of rat cerebral cortex membranes were characterized in binding. 2. Specific binding of [3H]-prazosin was saturable between 20-5000 pm. Scatchard plots of the binding data were non-linear, indicating the presence of two distinct affinity sites for prazosin (pKD, high = 10.1...

journal_title：British journal of pharmacology

authors： Oshita M,Kigoshi S,Muramatsu I

更新日期：1991-12-01 00:00:00

abstract：:1 Eleven analogues of sodium cromoglycate have been tested for their ability to suppress histamine release induced by anti-IgE from passively sensitized human lung fragments in vitro. 2 With the exception of WY 16922, which released histamine at high concentrations, all inhibited histamine release in a linear dose-rel...

journal_title：British journal of pharmacology

authors： Church MK,Gradidge CF

更新日期：1980-10-01 00:00:00

abstract：:1 The possible involvement of N-methyl-D-aspartate (NMDA)-receptors in epileptiform synaptic activity in the kainic acid (KA) lesioned hippocampus was investigated. In this chronic model of epilepsy there is a loss of both the early and the late components of synaptic inhibition as well as changes in the membrane prop...

journal_title：British journal of pharmacology

authors： Ashwood TJ,Wheal HV

更新日期：1987-08-01 00:00:00

abstract：:1. Two-electrode voltage clamp was used to study the effects of adenosine 3':5'-cyclic monophosphate (cyclic AMP) and guanosine 3':5'-cyclic monophosphate (cyclic GMP) on voltage-dependent ion channels in salivary gland cells of the leech, Haementeria ghilianii. 2. Intracellular cyclic AMP specifically blocked delayed...

journal_title：British journal of pharmacology

authors： Everill B,Berry MS

更新日期：1995-09-01 00:00:00

abstract：:Allergic inflammatory responses contribute to the symptoms of a number of diseases including atopic dermatitis, asthma and rhinitis. Cationic proteins are released from inflammatory cells and levels are known to be raised in disease states. Using an in vivo model of acute inflammation, we investigated the characterist...

journal_title：British journal of pharmacology

authors： Jones H,Paul W,Page CP

更新日期：2001-08-01 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：:We investigated whether 10 days' in vivo treatment with nitroglycerine (NTG) would inhibit nitric oxide production by the endothelial cells of resistance arteries ex vivo and, if so, what the underlying mechanism might be. ACh increased the intracellular nitric oxide concentration ([NO]i; estimated using the nitric ox...

journal_title：British journal of pharmacology

authors： Yamamoto T,Kajikuri J,Watanabe Y,Suzuki Y,Suzumori K,Itoh T

更新日期：2005-10-01 00:00:00

abstract：:1 The metabolism of extracellular nucleotides plays an important role in nucleotide signalling mediated by P2 receptors. The nucleotide sequence encoding a putative human ecto-ATPase named CD39L1 was reported recently. However, the biological activity of this protein has not been established. 2 Based on the sequence o...

journal_title：British journal of pharmacology

authors： Mateo J,Harden TK,Boyer JL

更新日期：1999-09-01 00:00:00

abstract：:1. [125I]-Tyr4-bombesin exhibited saturable binding to pancreatic acinar cells. 2. Preincubation of cells at 37 degrees C with 0.03 nM-1 microM-bombesin for 10 min followed by acid or neutral washes reduced subsequent binding of [125I]-Tyr4-bombesin in a concentration-dependent manner by up to 90%. 3. In cell suspensi...

journal_title：British journal of pharmacology

authors： Sjödin L,Gylfe E

更新日期：1994-08-01 00:00:00

abstract：:Des-Arg9-bradykinin (des-Arg9-BK) caused endothelium-dependent relaxations in human, isolated coronary arteries which upregulated with in vitro incubation time. Relaxations to des-Arg9-BK were inhibited by the B1 receptor antagonist, des-Arg9-[Leu3]-BK (pK(B), 6.14 +/- 0.11) but were unaffected by the B2 receptor anta...

journal_title：British journal of pharmacology

authors： Drummond GR,Cocks TM

更新日期：1995-12-01 00:00:00

abstract：:The oestrogenic and antioestrogenic activities of a series of substituted derivatives of 1,1,2 triphenylbut-1-ene have been determined using primary cultures of rat pituitary gland cells to monitor prolactin synthesis in vitro. The relative binding affinity of the agonists for the oestrogen receptor was consistent wit...

journal_title：British journal of pharmacology

authors： Jordan VC,Koch R,Mittal S,Schneider MR

更新日期：1986-01-01 00:00:00

abstract：:1. We have characterized the 5-hydroxytryptamine (5-HT)-induced calcium signalling in endothelial cells from the human pulmonary artery. Using RT-PCR we show, that of all cloned G-protein coupled 5-HT receptors, these cells express only 5-HT1D beta, 5-HT2B and little 5-HT4 receptor mRNA. 2. In endothelial cells 5-HT i...

journal_title：British journal of pharmacology

authors： Ullmer C,Boddeke HG,Schmuck K,Lübbert H

更新日期：1996-03-01 00:00:00

abstract：:1. The effect of the nootropic drug, piracetam on stress- and subsequent morphine-induced prolactin (PRL) secretion was investigated in vivo in male rats, by use of a stress-free blood sampling and drug administration method by means of a permanent indwelling catheter in the right jugular vein. 2. Four doses of pirace...

journal_title：British journal of pharmacology

authors： Matton A,Engelborghs S,Bollengier F,Finné E,Vanhaeist L

更新日期：1996-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:As a hallmark of glioblastoma multiforme (GBM), CD44 plays a crucial role in promoting glioblastoma stem cell (GSC) stemness phenotypes and multiple drug resistance. The therapeutic potential of CD44 has been validated by the clinical successes of several CD44 inhibitors, including antibodies and...

journal_title：British journal of pharmacology

authors： Wang C,Wang Z,Chen C,Fu X,Wang J,Fei X,Yan X,Xu R

更新日期：2020-07-01 00:00:00

abstract：:Mouse spiders represent a potential cause of serious envenomation in humans. This study examined the activity of Missulena bradleyi venom in several in vitro preparations. Whilst female M. bradleyi venom at doses up to 0.05 microl ml(-1) failed to alter twitch or resting tension in all preparations used, male venom (0...

journal_title：British journal of pharmacology

authors： Rash LD,Birinyi-Strachan LC,Nicholson GM,Hodgson WC

更新日期：2000-08-01 00:00:00

abstract：:Ginsenoside Rg1, an active ingredient in ginseng, was previously shown to be a novel class of potent phytoestrogen. The present study aims at investigating the molecular mechanisms involved in mediating its actions in human breast cancer (MCF-7) cells. Rg1 (1 pM) stimulates cell proliferation (P<0.01) and estrogen-res...

journal_title：British journal of pharmacology

authors： Chen WF,Lau WS,Cheung PY,Guo DA,Wong MS

更新日期：2006-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Chronic stress impairs GABAA (GABA type A) receptor-mediated inhibition in the hypothalamic paraventricular nucleus (PVN). It is not clear whether GABAB receptor function is also altered. We hypothesize that chronic stress alters GABAB receptor function in PVN corticotrophin-releasing hormone (CR...

journal_title：British journal of pharmacology

authors： Gao Y,Zhou JJ,Zhu Y,Wang L,Kosten TA,Zhang X,Li DP

更新日期：2017-09-01 00:00:00

abstract：:1. The effect of ondansetron, a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist, was studied in morphine-addicted rats. Morphine-dependence and tolerance, induced by drinking increasing concentrations of morphine sulphate in 5% sucrose solution for 3 weeks, were demonstrated by the naloxone-precipitated wit...

journal_title：British journal of pharmacology

authors： Hui SC,Sevilla EL,Ogle CW

更新日期：1996-06-01 00:00:00

abstract：:1 Release of [3H]-noradrenaline and 3H-purine by ouabain (10(-4)M) or high KCl (50 mM) was investigated in the superfused rabbit pulmonary arterial segment preincubated with [3H]-noradrenaline or [3H]-adenosine. 2 Ouabain elicited a delayed large contraction and a parallel [3H]-noradrenaline efflux. These were substan...

journal_title：British journal of pharmacology

authors： Katsuragi T,Su C

更新日期：1982-12-01 00:00:00

abstract：:1. OPC-31260, a benzazepine derivative, has been studied for its ability to antagonize the binding of arginine vasopressin (AVP) to receptors in rat liver (V1) and kidney (V2) plasma membranes, for antagonism of the antidiuretic action of AVP in alcohol-anaesthetized rats and for diuretic action in conscious normal ra...

journal_title：British journal of pharmacology

authors： Yamamura Y,Ogawa H,Yamashita H,Chihara T,Miyamoto H,Nakamura S,Onogawa T,Yamashita T,Hosokawa T,Mori T

更新日期：1992-04-01 00:00:00

abstract：:1. The effects of prejunctional beta-adrenoceptor activation on electrically evoked noradrenaline (NA) and adenosine 5'-triphosphate (ATP) were studied by use of continuous amperometry and conventional intracellular recording techniques. Excitatory junction potentials (e.j.ps) were used as a measure of ATP release, an...

journal_title：British journal of pharmacology

authors： Brock JA,Bridgewater M,Cunnane TC

更新日期：1997-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pelitinib is a potent irreversible EGFR TK inhibitor currently in clinical trials for the treatment of lung cancer. Hyperthermia has been applied concomitantly with chemotherapy and radiotherapy to enhance treatment outcome. In this study, we investigated the ability of the combination of pelitin...

journal_title：British journal of pharmacology

authors： To KK,Poon DC,Wei Y,Wang F,Lin G,Fu L

更新日期：2015-08-01 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：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：:1 The mechanism underlying the enhancement by superoxide dismutase (SOD) of endothelium-dependent relaxation was investigated in rabbit mesenteric resistance arteries. 2 SOD (200 U ml(-1)) increased the production of H(2)O(2) in smooth muscle cells (as indicated by the use of an H(2)O(2)-sensitive fluorescent dye). 3 ...

journal_title：British journal of pharmacology

authors： Itoh T,Kajikuri J,Hattori T,Kusama N,Yamamoto T

更新日期：2003-05-01 00:00:00