Binding of [3H]-muscimol, a potent gamma-aminobutyric acid receptor agonist, to membranes of the bovine retina.

abstract：:1. The possibility that tachykinin NK1 receptors are involved in the plasma extravasation evoked by intradermal (i.d.) injection of Phoneutria nigriventer venom (PNV) in rat dorsal skin in vivo has been investigated. 2. Local oedema formation induced by the i.d. injection of test agents was measured by the extravascul...

journal_title：British journal of pharmacology

authors： Palframan RT,Costa SK,Wilsoncroft P,Antunes E,de Nucci G,Brain SD

更新日期：1996-05-01 00:00:00

abstract：:1. The affinity of the alpha 1-adrenoceptor antagonist SB 216469 (also known as REC 15/2739) has been determined at native and cloned alpha 1-adrenoceptor subtypes by radioligand binding and at functional alpha 1-adrenoceptor subtypes in isolated tissues. 2. In radioligand binding studies with [3H]-prazosin, SB 216469...

journal_title：British journal of pharmacology

authors： Chess-Williams R,Chapple CR,Verfurth F,Noble AJ,Couldwell CJ,Michel MC

更新日期：1996-11-01 00:00:00

abstract：:1. Caffeine has been widely used as a pharmacological tool to evaluate Ca(2+) release from the sarcoplasmic reticulum in isolated smooth muscle cells. However, in nervous tissue this drug also causes neurotransmitters release, which might cause additional effects when smooth muscle strips are evaluated. To assess this...

journal_title：British journal of pharmacology

authors： Montaño LM,Carbajal V,Arreola JL,Barajas-López C,Flores-Soto E,Vargas MH

更新日期：2003-07-01 00:00:00

abstract：:Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment. In this study, the effects of TAK-147 at 2 mg kg(-1) p.o. for 21 days, compared t...

journal_title：British journal of pharmacology

authors： Hatip-Al-Khatib I,Iwasaki K,Yoshimitsu Y,Arai T,Egashira N,Mishima K,Ikeda T,Fujiwara M

更新日期：2005-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Screening of 12,000 compounds for binding affinity to the synaptic vesicle protein 2A (SV2A), identified a high-affinity pyrrolidone derivative, brivaracetam (ucb 34714). This study examined its pharmacological profile in various in vitro and in vivo models of seizures and epilepsy, to evaluate i...

journal_title：British journal of pharmacology

authors： Matagne A,Margineanu DG,Kenda B,Michel P,Klitgaard H

更新日期：2008-08-01 00:00:00

abstract：:1. TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin. It belongs to the transient receptor potential (TRP) family, and therefore is related to vanilloid receptor type-1 (VR1, TRPV1). We tested whether substances which are structurally related to ment...

journal_title：British journal of pharmacology

authors： Behrendt HJ,Germann T,Gillen C,Hatt H,Jostock R

更新日期：2004-02-01 00:00:00

abstract：:1. The central and peripheral effects of the omega (benzodiazepine) site ligands, clonazepam, alpidem, zolpidem, triazolam, flumazenil, ethyl beta carboline-3-carboxylate (beta-CCE) and N-methyl beta carboline-3-carboxylate (beta-CCM) on intestinal myoelectrical activity were evaluated in conscious rats, chronically f...

journal_title：British journal of pharmacology

authors： Bonnafous C,Scatton B,Buéno L

更新日期：1994-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:3,4-Methylenedioxymethamphetamine (MDMA or 'Ecstasy') is a worldwide major drug of abuse known to elicit neurotoxic effects. The mechanisms underlying the neurotoxic effects of MDMA are not clear at present, but the metabolism of dopamine and 5-HT by monoamine oxidase (MAO), as well as the hepati...

journal_title：British journal of pharmacology

authors： Barbosa DJ,Capela JP,Oliveira JM,Silva R,Ferreira LM,Siopa F,Branco PS,Fernandes E,Duarte JA,de Lourdes Bastos M,Carvalho F

更新日期：2012-02-01 00:00:00

abstract：:1. We examined the effects of eprosartan, an AT(1) receptor antagonist, on the progression of left ventricular (LV) dysfunction and remodelling in dogs with heart failure (HF) produced by intracoronary microembolizations (LV ejection fraction, EF 30 to 40%). 2. Dogs were randomized to 3 months of oral therapy with low...

journal_title：British journal of pharmacology

authors： Suzuki G,Mishima T,Tanhehco EJ,Sharov VG,Todor A,Rostogi S,Gupta RC,Chaudhry PA,Anagnostopoulos PV,Nass O,Goldstein S,Sabbah HN

更新日期：2003-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is increasing evidence that angiotensin II (Ang II) is associated with the occurrence of ventricular arrhythmias. However, little is known about the electrophysiological effects of Ang II on ventricular repolarization. The rapid component of the delayed rectifier K(+) current (I(Kr)) plays ...

journal_title：British journal of pharmacology

authors： Wang YH,Shi CX,Dong F,Sheng JW,Xu YF

更新日期：2008-05-01 00:00:00

abstract：:1. We have examined the mechanisms by which the K(+)-channel blocker 4-aminopyridine (4-AP) can dose-dependently increase both basal [3H]-noradrenaline ([3H]-NA) release and the [3H]-NA release evoked by electrical stimulation, but not the release of [3H]-acetylcholine ([3H]-ACh), from slices of rat hippocampus. 2. Bo...

journal_title：British journal of pharmacology

authors： Hu PS,Fredholm BB

更新日期：1991-03-01 00:00:00

abstract：:1. The mechanism of the inhibitory effect of dehydroemetine on the heart was investigated using (a) the spontaneously contracting isolated guinea-pig atrial preparation and (b), the electrically driven left atrial preparation.2. Dehydroemetine decreased the rate and amplitude of contraction of spontaneously contractin...

journal_title：British journal of pharmacology

authors： Salako LA

更新日期：1972-12-01 00:00:00

abstract：:The properties of the ATPase released during electrical field stimulation (EFS) (8 Hz, 25 s) of the sympathetic nerves of the superfused rabbit isolated vas deferens were investigated. Superfusate collected during EFS rapidly metabolised exogenous ATP (100 microM) and 50% was broken down in 5.67+/-0.65 min. The main m...

journal_title：British journal of pharmacology

authors： Westfall TD,Menzies JR,Liberman R,Waterston S,Ramphir N,Westfall DP,Sneddon P,Kennedy C

更新日期：2000-11-01 00:00:00

abstract：:Following the discovery of the first effective antiviral compound (idoxuridine) in 1959, nucleoside analogues, especially acyclovir (ACV) for the treatment of herpesvirus infections, have dominated antiviral therapy for several decades. However, ACV and similar acyclic nucleosides suffer from low aqueous solubility an...

journal_title：British journal of pharmacology

authors： De Clercq E,Field HJ

更新日期：2006-01-01 00:00:00

abstract：:1. Immunized BP2 mice developed an acute bronchoconstriction in vivo and airway muscle contraction in vitro in response to ovalbumin (OA) and these contractions were dose dependent. 2. Methysergide or atropine inhibited OA-induced bronchoconstriction in vivo and airway muscle contraction in vitro. 3. Neostigmine poten...

journal_title：British journal of pharmacology

authors： Eum SY,Norel X,Lefort J,Labat C,Vargaftig BB,Brink C

更新日期：1999-01-01 00:00:00

abstract：:1. Experiments were performed with peptidase inhibitors on rabbit aortic strip preparations, to determine whether endogenous peptidase activity can influence the potency estimates for angiotensin receptor agonists and antagonists in this tissue. 2. Angiotensin II (A II) and angiotensin III (A III) both induced concent...

journal_title：British journal of pharmacology

authors： Robertson MJ,Cunoosamy MP,Clark KL

更新日期：1992-05-01 00:00:00

abstract：:1 The concentrations of p- and m-tyramine were measured in the caudate nucleus of the rat brain following subcutaneous injection of reserpine or intraventricular injection of 6-hydroxydopamine, beta-Phenylethylamine was analysed in the hypothalamus after reserpine. 2 Endogenous levels of p-tyramine and m-tyramine in t...

journal_title：British journal of pharmacology

authors： Boulton AA,Juorio AV,Philips SR,Wu PH

更新日期：1977-01-01 00:00:00

abstract：:Arterial stiffness progressively increases with aging and is an independent predictor of cardiovascular disease (CVD) risk. Evidence supports that there are sex differences in the time course of aging-related arterial stiffness and the associated CVD risk, which increases disproportionately in postmenopausal women. Th...

journal_title：British journal of pharmacology

authors： DuPont JJ,Kenney RM,Patel AR,Jaffe IZ

更新日期：2019-11-01 00:00:00

abstract：:1. alpha 1-Adrenoceptor subtypes in rabbit thoracic aorta have been examined in binding and functional experiments. 2. [3H]-prazosin bound to two distinct populations of alpha 1-adrenoceptors (pKD,high = 9.94, Rhigh = 79.2 fmol mg-1 protein; pKD,low = 8.59, Rlow = 215 fmol mg-1 protein). Pretreatment with chloroethylc...

journal_title：British journal of pharmacology

authors： Oshita M,Kigoshi S,Muramatsu I

更新日期：1993-04-01 00:00:00

abstract：:Cellular electrophysiological effects of membrane lipid peroxidation by t-butyl hydroperoxide (TBH) were studied in the rabbit sinoatrial (SA) node. Superfusion for 1-5 min with 300 microM TBH caused an initial increase and subsequent decrease in the spontaneous firing frequency of the SA node. Voltage clamp experimen...

journal_title：British journal of pharmacology

authors： Sato N,Nishimura M,Tanaka H,Homma N,Watanabe Y

更新日期：1989-11-01 00:00:00

abstract：:Rat vas deferens preparations became desensitized to the alpha 1-adrenoceptor antagonist thymoxamine: after 6 h in vitro, the t 1/2 value (time to attain half the occupancy of receptors occupied at equilibrium) of the response to this drug was 1.50 fold greater in control strips (strips exposed to thymoxamine at 6 h) ...

journal_title：British journal of pharmacology

authors： Onnen I

更新日期：1984-09-01 00:00:00

abstract：:Oxidized low density lipoproteins (oxLDL) are thought to play a major role in atherosclerosis. OxLDL act in part through alteration of intracellular signalling pathways in cells of the vascular wall. We recently reported that the EGF receptor (EGFR) signalling pathway is activated by lipid peroxidation products (among...

journal_title：British journal of pharmacology

authors： Vacaresse N,Vieira O,Robbesyn F,Jürgens G,Salvayre R,Negre-Salvayre A

更新日期：2001-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhalation of the superantigen,staphylococcal enterotoxin B (SEB), leads to the activation of the host T and invariant natural killer (iNK) T cells, thereby resulting in acute lung inflammation and respiratory failure but the underlying mechanism(s) of disease remain elusive, with limited treatme...

journal_title：British journal of pharmacology

authors： Rieder SA,Nagarkatti P,Nagarkatti M

更新日期：2012-11-01 00:00:00

abstract：:1. We investigated the potent 5-hydroxytryptamine (5-HT)-mediated vasorelaxation of the sheep pulmonary vein. Here we present evidence that this response is due to activation of 5-HT4 receptors. 2. 5-HT (1-1000 nM) caused concentration-dependent, maintained relaxations (pEC50 = 8.4 +/- 0.1) of isolated rings of sheep ...

journal_title：British journal of pharmacology

authors： Cocks TM,Arnold PJ

更新日期：1992-10-01 00:00:00

abstract：:We investigated the effects of cocaine and corticosterone on the noradrenaline-induced relaxation of rat oesophageal smooth muscle in the absence and presence of the selective beta2-antagonist, ICI 111,551. It was found that the concentration-response curve (CRC) of noradrenaline was not shifted by ICI 118,551 at 1 mi...

journal_title：British journal of pharmacology

authors： de Boer RE,Brouwer F,Zaagsma J

更新日期：1995-10-01 00:00:00

abstract：:1. The subtype of alpha1-adrenoceptor mediating contractions to phenylephrine of the rat thoracic aorta, mesenteric artery and pulmonary artery were investigated by use of antagonists which show selectivity between the cloned alpha1-adrenoceptor subtypes in binding studies. 2. Cumulative concentration-contraction curv...

journal_title：British journal of pharmacology

authors： Hussain MB,Marshall I

更新日期：1997-11-01 00:00:00

abstract：:An increasing number of examples in the literature suggest that the in vivo duration of drug action not only depends on macroscopic pharmacokinetic properties like plasma half-life and the time needed to equilibrate between the plasma and the effect compartments, but is also influenced by long-lasting target binding a...

journal_title：British journal of pharmacology

authors： Vauquelin G,Charlton SJ

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pulmonary hypertension (PH) is a devastating disease characterized by increased pulmonary arterial pressure, which progressively leads to right-heart failure and death. A dys-regulated renin angiotensin system (RAS) has been implicated in the development and progression of PH. However, the role o...

journal_title：British journal of pharmacology

authors： Bruce E,Shenoy V,Rathinasabapathy A,Espejo A,Horowitz A,Oswalt A,Francis J,Nair A,Unger T,Raizada MK,Steckelings UM,Sumners C,Katovich MJ

更新日期：2015-05-01 00:00:00

abstract：:1. Characterization of the beta-adrenoceptors mediating inhibition of gastric acid secretion in the conscious Heidenhain pouch dog has been investigated by determination of the effects of propranolol, (+)-propranolol, practolol and H35/25 on salbutamol and isoprenaline-induced inhibition of gastric acid secretion. 2. ...

journal_title：British journal of pharmacology

authors： Daly MJ,Long JM,Stables R

更新日期：1978-09-01 00:00:00

abstract：:1. The effect of the myorelaxant drugs baclofen, diazepam and tizanidine have been compared on in vitro preparations of baby rat spinal cord and adult rat superior cervical ganglion. 2. Dorsal root-elicited long duration (time to half decay 9.71 +/- 0.29 s.e. mean, n = 31) ipsilateral ventral root reflexes (DR-VRP), m...

journal_title：British journal of pharmacology

authors： Siarey RJ,Long SK,Evans RH

更新日期：1992-10-01 00:00:00