Dopamine receptor-mediated spinal antinociception in the normal and haloperidol pretreated rat: effects of sulpiride and SCH 23390.

abstract：:Knowledge of the cardiac safety of emerging new drugs is an important aspect of assuring the expeditious advancement of the best candidates targeted at unmet medical needs while also assuring the safety of clinical trial subjects or patients. Present methodologies for assessing drug-induced torsades de pointes (TdP) a...

journal_title：British journal of pharmacology

authors： Bass AS,Darpo B,Breidenbach A,Bruse K,Feldman HS,Garnes D,Hammond T,Haverkamp W,January C,Koerner J,Lawrence C,Leishman D,Roden D,Valentin JP,Vos MA,Zhou YY,Karluss T,Sager P

更新日期：2008-08-01 00:00:00

abstract：:1. In pithed rats, preganglionic vagal nerve stimulation (at 5 Hz) elicited a bradycardia. This bradycardia was potentiated by the angiotensin converting enzyme inhibitor, captopril (1 mg kg-1, i.v.) by about 40%. Subsequent angiotensin II infusion (0.03 micrograms kg-1 min-1) reversed this effect. A similar facilitat...

journal_title：British journal of pharmacology

authors： Rechtman M,Majewski H

更新日期：1993-09-01 00:00:00

abstract：:1. Bicyclic compounds with potential thymoleptic properties (Lu-compounds) have recently become available, and their effects on the membrane pumps of the central and peripheral monoamine neurones have now been tested and compared with those of the tricyclic antidepressant drugs.2. Biochemical and histochemical in vivo...

journal_title：British journal of pharmacology

authors： Carlsson A,Fuxe K,Hamberger B,Malmfors T

更新日期：1969-05-01 00:00:00

abstract：:1. The present study has compared the relative anti-aggregatory effect of various compounds which interfere with thromboxane (Tx) A2-dependent aggregation of human platelets in whole blood in vitro. These included the cyclo-oxygenase inhibitor aspirin, the TxA2 synthase inhibitor dazoxiben, the TxA2 (TP-) receptor blo...

journal_title：British journal of pharmacology

authors： Watts IS,Wharton KA,White BP,Lumley P

更新日期：1991-02-01 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：:1. Dogs, anaesthetized with chloralose and urethane, were subjected to a 25 min occlusion of the left anterior descending coronary artery. This resulted in ventricular ectopic activity, a reduction in baroreflex sensitivity (BRS, measured following the intravenous administration of phenylephrine), elevations in the ep...

journal_title：British journal of pharmacology

authors： Babai L,Papp JG,Parratt JR,Végh A

更新日期：2002-01-01 00:00:00

abstract：:Adenosine alone at 0.1 and 1.0 mg per tracheal segment stimulated mucus secretion by 52% and 88%, respectively, compared to baseline (P less than 0.0001). The site of the potent secretagogue effect of adenosine in canine trachea was consistent with A2 activation. A2 site activation and enhanced secretion were also ind...

journal_title：British journal of pharmacology

authors： Johnson HG,McNee ML

更新日期：1985-09-01 00:00:00

abstract：:1 Prolonged exposure (6-12 h) of rat aorta to alpha1-adrenergic receptor (alpha(1)AR) agonist phenylephrine (Phe) leads to a decrease in alpha(1)AR-mediated vasoconstriction. This reduced responsiveness to alpha(1)AR stimulation was strongly dependent on the intactness of the endothelium. 2 We examined the effect of P...

journal_title：British journal of pharmacology

authors： Gürdal H,Can A,Uğur M

更新日期：2005-05-01 00:00:00

abstract：:1. Imidazoline binding sites have been reported to be present in the locus coeruleus (LC). To investigate the role of these sites in the control of LC neuron activity, we studied the effect of imidazolines using in vivo and in vitro single-unit extracellular recording techniques. 2. In anaesthetized rats, local (27 pm...

journal_title：British journal of pharmacology

authors： Ugedo L,Pineda J,Ruiz-Ortega JA,Martín-Ruiz R

更新日期：1998-12-01 00:00:00

abstract：:The effects of intravenous doses of Org 6001 and disopyramide (10 mg/kg) known to confer protection against early postligation-induced arrhythmias in the anaesthetized rat when given prophylactically, were assessed following postligation administration. When given 1 min after ligation both drugs greatly reduced the in...

journal_title：British journal of pharmacology

authors： Marshall RJ,Muir AW,Winslow E

更新日期：1982-08-01 00:00:00

abstract：:Despite progression in anticancer drug development and improvements in the clinical utilization of therapies, current treatment regimes are still dependent upon the use of systemic antiproliferative cytotoxic agents. Although these agents are unquestionably potent, their efficacy is limited by toxicity towards 'normal...

journal_title：British journal of pharmacology

authors： Atkinson JM,Siller CS,Gill JH

更新日期：2008-04-01 00:00:00

abstract：:1. Enprostil is composed, in approximately equal proportions, of 4 allenic isomers which are prostanoids structurally related to prostaglandin E2 (PGE2). The isomers are denoted as RS-86505-007, RS-86812-007 which are in the 'natural' R and S configuration (with respect to PGE2) and RS-86505-008 and RS-86812-008 which...

journal_title：British journal of pharmacology

authors： Eglen RM,Whiting RL

更新日期：1989-12-01 00:00:00

abstract：:1 U46619, a prostaglandin H2 endoperoxide analogue and thromboxane A2 agonist, dose-dependently inhibited accumulation and metabolism of thromboxane B2 in the isolated perfused lung of the guinea-pig. At similar doses prostaglandins E1, E2, F1 alpha, F2 alpha, I2, 5, 6-trans-PGE2 and 8-iso-PGE1 were ineffective. 2 U46...

journal_title：British journal of pharmacology

authors： Hoult JR,Robinson C

更新日期：1983-01-01 00:00:00

abstract：:1. A crude preparation of toxin was extracted from a sample of mussels Mytilus edulis, part of a batch responsible for many cases of paralytic shellfish poisoning.2. The crude extract was partially purified by absorption on sodium Amberlite ion-exchange resin. Two toxins were recovered by elution from the Amberlite, a...

journal_title：British journal of pharmacology

authors： Evans MH

更新日期：1970-12-01 00:00:00

abstract：:1. We assessed the relaxant effect of 17 beta-oestradiol (10(-7), 10(-6) and 10(-5) M) on rabbit isolated coronary arteries precontracted with prostaglandin F2 alpha (3 x 10(-6) M), high extracellular potassium (30 mM) and Bay K 8644 (10(-6) M) plus high extracellular potassium (15 mM) by measuring isometric tension. ...

journal_title：British journal of pharmacology

authors： Jiang CW,Sarrel PM,Lindsay DC,Poole-Wilson PA,Collins P

更新日期：1991-12-01 00:00:00

abstract：:1. The action of adrenaline on the K(+) balance of the isolated heart was found to depend on the ionic composition and the temperature of the perfusion fluids used.2. When the perfusion fluid contained 145 mM Na(+), 1.7 mM Ca(++) and 3-9 mM K(+), adrenaline caused the hearts to gain K(+); when the K(+) concentration w...

journal_title：British journal of pharmacology

authors： Stafford A

更新日期：1969-07-01 00:00:00

abstract：:1. The effects of 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), an inhibitor of soluble guanylyl cyclase (sGC), were investigated in aortic rings and ventricular cardiomyocytes from rats. The production of cyclic GMP was stimulated by NO.-donors or carbachol. Additionally, the effects of ODQ were studied in cytos...

journal_title：British journal of pharmacology

authors： Wegener JW,Closs EI,Förstermann U,Nawrath H

更新日期：1999-06-01 00:00:00

abstract：:1. The binding of 2-[125I]-iodomelatonin to chicken brain membranes, and the inhibition of binding by melatonin, N-acetyltryptamine and luzindole, were examined at temperatures between 4 degrees C and 37 degrees C. 2. At all temperatures studied, the binding affinity (Kd or Ki) for 2-[125I]-iodomelatonin, melatonin (b...

journal_title：British journal of pharmacology

authors： Chong NW,Sugden D

更新日期：1994-01-01 00:00:00

abstract：:1. The neurotransmitters involved in NANC relaxation and their possible interactions were investigated in mouse isolated stomach, recording the motor responses as changes of endoluminal pressure from whole organ. 2. Field stimulation produced tetrodotoxin-sensitive, frequency-dependent, biphasic responses: rapid trans...

journal_title：British journal of pharmacology

authors： Mulè F,Serio R

更新日期：2003-09-01 00:00:00

abstract：:1. In order to investigate the vasodilator mechanisms of the K+ channel openers, cromakalim, pinacidil and nicorandil, we measured changes in cytoplasmic Ca2+ concentration [( Ca2+]i) simultaneously with force by a microfluorimetric method using fura-2, a calcium indicator, in canine coronary arterial smooth muscle ce...

journal_title：British journal of pharmacology

authors： Yanagisawa T,Teshigawara T,Taira N

更新日期：1990-09-01 00:00:00

abstract：:1 Pinacidil relaxes blood vessels through opening the K(ATP) channels with a resultant membrane hyperpolarization and inhibition of Ca(2+) influx. The aim of this study was to examine the mechanisms thereby pinacidil induces K(+) channel-independent relaxation in isolated endothelium-denuded rat mesenteric artery. 2 P...

journal_title：British journal of pharmacology

authors： Tsang SY,Yao X,Wong CM,Au CL,Chen ZY,Huang Y

更新日期：2003-02-01 00:00:00

abstract：:1. The modulation of L-type calcium channel current (ICa) by fendiline, a diphenylalkylamine type of calcium channel blocker was investigated on guinea-pig ventricular myocytes by use of the whole-cell patch-clamp technique. 2. Fendiline-induced block of ICa is accompanied by modulation of the channel kinetics in a co...

journal_title：British journal of pharmacology

authors： Schreibmayer W,Tripathi O,Tritthart HA

更新日期：1992-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-arachidonoyl 5-HT (NA-5HT) has anti-nociceptive effects reported to be mediated by inhibitory actions at the transient receptor potential vanilloid receptor 1 (TRPV1) and fatty acid amide hydrolase (FAAH). Anandamide and N-arachidonoyl dopamine (NA-DA), endocannabinoids that activate TRPV1 or a...

journal_title：British journal of pharmacology

authors： Gilmore AJ,Heblinski M,Reynolds A,Kassiou M,Connor M

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Extrahepatic vasodilation and increased intrahepatic vascular resistance represent attractive targets for the medical treatment of portal hypertension in liver cirrhosis. In both dysfunctions, dysregulation of the contraction-mediating Rho kinase plays an important role as it contributes to alter...

journal_title：British journal of pharmacology

authors： Hennenberg M,Trebicka J,Stark C,Kohistani AZ,Heller J,Sauerbruch T

更新日期：2009-05-01 00:00:00

abstract：:1. The effects of adrenaline, noradrenaline, isoprenaline and terbutaline (PINN), 1-(3,5-dihydroxyphenyl)-2(t-butylamino)-ethanol, on the sphincter of Oddi were studied in anaesthetized cats. Both adrenaline and noradrenaline (1-4 mug/kg) increased resistance to flow through the sphincter. This effect was blocked by d...

journal_title：British journal of pharmacology

authors： Liedberg G,Persson CG

更新日期：1970-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

journal_title：British journal of pharmacology

authors： Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

更新日期：2012-09-01 00:00:00

abstract：:1. The effect of the nitro-derivative of aspirin, NCX4016, was assessed on ischaemic ventricular arrhythmias and myocardial infarct size in anaesthetized pigs in comparison to native aspirin. 2. Pigs were given aspirin (10 mg kg(-1); n=6), low dose NCX4016 (18.4 mg kg(-1); n=6) or high dose NCX4016 (60 mg kg(-1); n=7)...

journal_title：British journal of pharmacology

authors： Wainwright CL,Miller AM,Work LM,Del Soldato P

更新日期：2002-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Glucagon-like peptide-1 (GLP-1) is an incretin hormone that regulates insulin biosynthesis and secretion in a glucose-dependent manner and has been reported to induce vasodilatation. Here, we examined the possible vasorelaxant effect of GLP-1 and its underlying mechanisms. EXPERIMENTAL APPROACH:...

journal_title：British journal of pharmacology

authors： Bangshaab M,Gutierrez A,Huynh KD,Knudsen JS,Arcanjo DDR,Petersen AG,Rungby J,Gejl M,Simonsen U

更新日期：2019-02-01 00:00:00

abstract：:1. The aim of the present study was to examine whether ramipril induces delayed myocardial protection against free radical injuries ex vivo and to determine the possible role of the bradykinin B2-nitric oxide (NO) pathway, prostaglandins(PGs) and protein synthesis in this delayed adaptive response. 2. Rats were pretre...

journal_title：British journal of pharmacology

authors： Jin ZQ,Chen X

更新日期：1998-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:A non-psychoactive phytocannabinoid, cannabidiol (CBD), shows promising results as an effective potential antiepileptic drug in some forms of refractory epilepsy. To elucidate the mechanisms by which CBD exerts its anti-seizure effects, we investigated its effects at synaptic connections and on t...

journal_title：British journal of pharmacology

authors： Khan AA,Shekh-Ahmad T,Khalil A,Walker MC,Ali AB

更新日期：2018-06-01 00:00:00