Modulation of histamine H(2) receptor signalling by G-protein-coupled receptor kinase 2 and 3.

abstract：:1. The present study was designed to evaluate the nature of intervening agents in L-DOPA- and dopamine-induced neurotoxicity in Neuro-2A cells. 2. In the absence of cells and in conditions of light protection, at 37 degrees C, L-DOPA or dopamine (1 mM) in culture medium degraded spontaneously in a time-dependent manne...

journal_title：British journal of pharmacology

authors： Pedrosa R,Soares-da-Silva P

更新日期：2002-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Transient receptor potential canonical 5 (TRPC5) channels are widely expressed, including in the CNS, where they potentiate fear responses. They also contribute to other non-selective cation channels that are stimulated by G-protein-coupled receptor agonists and lipid and redox factors. Steroids ...

journal_title：British journal of pharmacology

authors： Majeed Y,Amer MS,Agarwal AK,McKeown L,Porter KE,O'Regan DJ,Naylor J,Fishwick CW,Muraki K,Beech DJ

更新日期：2011-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Psychological stress exacerbates symptoms of urinary bladder dysfunction; however, the underlying brain mechanisms are unclear. We have demonstrated that centrally administered bombesin, a stress-related neuropeptide, facilitates the rat micturition reflex. Brain bombesin-like peptides modulate t...

journal_title：British journal of pharmacology

authors： Shimizu T,Shimizu S,Wada N,Takai S,Shimizu N,Higashi Y,Kadekawa K,Majima T,Saito M,Yoshimura N

更新日期：2017-09-01 00:00:00

abstract：:1 Histamine produced a dose-dependent contraction of the isolated portal vein of the rabbit. This contraction was not antagonized by atropine, methysergide, indomethacin, cocaine or 6-hydroxy-dopamine, nor by pretreatment of the rabbit with reserpine. 2 The response to histamine was blocked by H1-receptor antagonists ...

journal_title：British journal of pharmacology

authors： Cook DA,Macleod KM

更新日期：1978-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In terms of postjunctional alpha(2)-adrenoceptors in the pulmonary circulation, no evidence is available with regard to the receptor subtypes mediating vasoconstriction. Therefore, we characterized the alpha(2)-adrenoceptor subtypes mediating contraction in isolated porcine pulmonary veins. EXPE...

journal_title：British journal of pharmacology

authors： Görnemann T,von Wenckstern H,Kleuser B,Villalón CM,Centurión D,Jähnichen S,Pertz HH

更新日期：2007-05-01 00:00:00

abstract：:1. The use of pharmacological inhibitors of nitric oxide (NO) synthesis to treat patients with septic shock is limited by the observation that they cause a fall in cardiac output in some subjects. The aim of this work was to investigate this fall and to test whether it was reversible by subsequent administration of ni...

journal_title：British journal of pharmacology

authors： Herity NA,Allen JD,Silke B,Adgey AA

更新日期：1994-06-01 00:00:00

abstract：:Nebivolol, a selective beta-adrenoceptor (beta1-AR) antagonist, induces vasodilatation by an endothelium- and NO-cGMP-dependent pathway. However, the mechanisms involved in the vascular effect of nebivolol have not been established. Thus, we evaluated the role of alpha1 and beta3-ARs in nebivolol-induced vasodilatatio...

journal_title：British journal of pharmacology

authors： Rozec B,Quang TT,Noireaud J,Gauthier C

更新日期：2006-04-01 00:00:00

abstract：:1. In this study, we compared two series of newly discovered ligands for their selectivity to benzodiazepine sites in the alpha 1 beta 2 gamma 2 and the alpha 6 beta 2 gamma 2 subtypes of cloned gamma-aminobutyric acidA (GABAA) receptors, the latter being unique in not interacting with classical benzodiazepines. 2. Th...

journal_title：British journal of pharmacology

authors： Im WB,Im HK,Pregenzer JF,Hamilton BJ,Carter DB,Jacobsen EJ,TenBrink RE,VonVoigtlander PF

更新日期：1993-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:QT prolongation is commonly used as a surrogate marker for Torsade de Pointes (TdP) risk of non-cardiovascular drugs. However, use of this indirect marker often leads to misinterpretation of the realistic TdP risk, as tested compounds may cause QT prolongation without evoking TdP in humans. A neg...

journal_title：British journal of pharmacology

authors： Guns PJ,Johnson DM,Van Op den Bosch J,Weltens E,Lissens J

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Antiretroviral (ARV) drugs activate pregnane X receptors and constitutive androstane receptors, increasing the risk of drug interactions due to altered drug metabolism and disposition. The closely related liver X receptors (LXRα/β), oestrogen receptors (ERα/β) and glucocorticoid receptor (GR) reg...

journal_title：British journal of pharmacology

authors： Svärd J,Blanco F,Nevin D,Fayne D,Mulcahy F,Hennessy M,Spiers JP

更新日期：2014-01-01 00:00:00

abstract：:Athletes attempt to improve performance with drugs that act on the beta-adrenergic system directly or indirectly. Of three beta-adrenoceptor (AR) subtypes, the beta(2)-AR is the main target in sport; they have bronchodilator and anabolic actions and enhance anti-inflammatory actions of corticosteroids. Although demons...

journal_title：British journal of pharmacology

authors： Davis E,Loiacono R,Summers RJ

更新日期：2008-06-01 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. Steady state fever has been produced in rabbits with a priming injection followed by a sustaining infusion of homologous plasma containing endogenous pyrogen (EP). This fever appears to last as long as the infusion continues.2. Intravenous salicylate given 1 h after the start of the EP infusion produced only a smal...

journal_title：British journal of pharmacology

authors： Cranston WI,Luff RH,Rawlins MD,Wright VA

更新日期：1971-02-01 00:00:00

abstract：:1 Sheep were injected with either methotrexate or melphalan in an attempt to lower the numbers of neutrophil granulocytes in peripheral blood. 2 Methotrexate, 5.0 mg/kg intravenously, on three consecutive days, produced no noticeable clinical or haematological changes. 3 A single dose of melphalan, 1.0 mg/kg intraveno...

journal_title：British journal of pharmacology

authors： Greenwood B,Kerry PJ

更新日期：1978-06-01 00:00:00

abstract：:1. The effects of suramin on an adenosine 5'-triphosphate (ATP)-activated inward current were investigated in PC12 phaeochromocytoma cells with whole-cell voltage-clamp techniques. 2. Suramin (30 to 300 microM) inhibited the ATP-activated current in a dose-dependent manner. The inhibitory effects were reversible and c...

journal_title：British journal of pharmacology

authors： Nakazawa K,Fujimori K,Takanaka A,Inoue K

更新日期：1990-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The passage of drugs across the blood-brain barrier (BBB) limits the efficacy of chemotherapy in brain tumours. For instance, the anticancer drug doxorubicin, which is effective against glioblastoma in vitro, has poor efficacy in vivo, because it is extruded by P-glycoprotein (Pgp/ABCB1), multidr...

journal_title：British journal of pharmacology

authors： Pinzón-Daza M,Garzón R,Couraud P,Romero Ia,Weksler B,Ghigo D,Bosia A,Riganti C

更新日期：2012-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:This paper is intended to assist pharmacologists to make the most of statistical analysis and in avoid common errors. APPROACH:A scenario is presented where an experimenter performed an experiment to test the effects of two drugs on cultured cells. Analysis of the results, expressed as percentag...

journal_title：British journal of pharmacology

authors： Lew M

更新日期：2007-10-01 00:00:00

abstract：:1. The aim of this study was to investigate whether the hypotensive effect of rat alpha-calcitonin gene-related peptide (alpha CGRP) in conscious rats is mediated by endothelium-derived nitric oxide (NO) or the opening of adenosine 5'-triphosphate (ATP)-sensitive potassium (KATP) channels. 2. Dose-mean arterial pressu...

journal_title：British journal of pharmacology

authors： Abdelrahman A,Wang YX,Chang SD,Pang CC

更新日期：1992-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:This study represents a novel characterisation of KCNQ-encoded potassium channels in the vasculature using a variety of pharmacological and molecular tools to determine their role in contractility. EXPERIMENTAL APPROACH:Reverse transcriptase polymerase chain reaction (RT-PCR) experiments were un...

journal_title：British journal of pharmacology

authors： Yeung SY,Pucovský V,Moffatt JD,Saldanha L,Schwake M,Ohya S,Greenwood IA

更新日期：2007-07-01 00:00:00

abstract：:(1) Stimulation of the vanilloid receptor-1 (TRPV1) results in the activation of nociceptive and neurogenic inflammatory responses. Poor specificity and potency of TRPV1 antagonists has, however, limited the clarification of the physiological role of TRPV1. (2) Recently, iodo-resiniferatoxin (I-RTX) has been reported ...

journal_title：British journal of pharmacology

authors： Rigoni M,Trevisani M,Gazzieri D,Nadaletto R,Tognetto M,Creminon C,Davis JB,Campi B,Amadesi S,Geppetti P,Harrison S

更新日期：2003-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pancreatic cancer is characterized by alterations in several key signalling proteins, including increased expression and activity of the Src tyrosine kinase and focal adhesion kinase (FAK), which have been linked to its chemoresistance. Sustained Src inhibition reactivates survival pathways regul...

journal_title：British journal of pharmacology

authors： Pathania D,Kuang Y,Sechi M,Neamati N

更新日期：2015-01-01 00:00:00

abstract：:Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs). Agonist affinity may be estimated in terms of the dissociation const...

journal_title：British journal of pharmacology

authors： Strange PG

更新日期：2008-04-01 00:00:00

abstract：:The novel urotensin-II (U-II) receptor (UT) ligand, [Pen(5),DTrp(7),Dab(8)]U-II(4-11) (UFP-803), was pharmacologically evaluated and compared with urantide in in vitro and in vivo assays. In the rat isolated aorta, UFP-803 was inactive alone but, concentration dependently, displaced the contractile response to U-II to...

journal_title：British journal of pharmacology

authors： Camarda V,Spagnol M,Song W,Vergura R,Roth AL,Thompson JP,Rowbotham DJ,Guerrini R,Marzola E,Salvadori S,Cavanni P,Regoli D,Douglas SA,Lambert DG,Calò G

更新日期：2006-01-01 00:00:00

abstract：:1 Amodiaquine was found to be a potent inhibitor in vitro of gastric histamine methyltransferase from human and canine corpus and from pig antrum. The ID50 for the enzyme, purified from pig antrum mucosa by ultracentrifugation and chromatography on DEAE-cellulose, was 2.5 muM. 2 In six dogs with Heidenhanin pouches th...

journal_title：British journal of pharmacology

authors： Barth H,Lorenz W,Troidl H

更新日期：1975-11-01 00:00:00

abstract：:1. In rat aortic rings contracted by phenylephrine, the relaxation induced by isoprenaline was partly inhibited by iberiotoxin, (ibTX), tetraethylammonium, 4-aminopyridine (4-AP) and 1,9-dideoxyforskolin, but not by glibenclamide. 2. In the presence of 4-AP, 1,9-dideoxyforskolin failed to inhibit further the relaxant ...

journal_title：British journal of pharmacology

authors： Satake N,Shibata M,Shibata S

更新日期：1996-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Stress is believed to be associated with the development of neuropsychiatric disorders, including Alzheimer's disease (AD). We have studied mechanisms implicated in vulnerability to stress and the relationship with changes in AD-related markers. EXPERIMENTAL APPROACH:Anhedonia induced by a chron...

journal_title：British journal of pharmacology

authors： Briones A,Gagno S,Martisova E,Dobarro M,Aisa B,Solas M,Tordera R,Ramírez M

更新日期：2012-02-01 00:00:00

abstract：:The effects of 15-hydroperoxy metabolites of arachidonic acid on vascular tone were evaluated in the perfused mesenteric preparation, the isolated perfused lung and segments of pulmonary arteries of the rat. In the mesenteric preparation, precontracted with phenylephrine, both 15-hydroperoxy-5,8,11,13-eicosatetraenoic...

journal_title：British journal of pharmacology

authors： d'Alarcao M,Corey EJ,Cunard C,Ramwell P,Uotila P,Vargas R,Wroblewska B

更新日期：1987-07-01 00:00:00

abstract：:1. Cannabinoids are potent inhibitors of endothelium-derived hyperpolarizing factor (EDHF)-mediated relaxations. We set out to study the mechanism underlying this effect and the possible role of cannabinoid-induced changes in intercellular gap junction communication. 2. In cultured endothelial cells, Delta(9)-tetrahyd...

journal_title：British journal of pharmacology

authors： Brandes RP,Popp R,Ott G,Bredenkötter D,Wallner C,Busse R,Fleming I

更新日期：2002-07-01 00:00:00

abstract：:1 Citrated platelet-rich plasma was prepared from New Zealand white rabbits before, during and after administration of chlorpromazine (2 mg/kg) intramuscularly once daily for 3 to 4 weeks. 2 In these plasmas, the velocity of platelet aggregation by 5-hydroxytryptamine (5-HT) added at 1, 3 and 10 microM increased great...

journal_title：British journal of pharmacology

authors： Baldacci M,Baldacci M,Bergel TD,Born GV,Hickman M

更新日期：1980-05-01 00:00:00

abstract：:1. Bradykinin (BK) instilled directly into the airway lumen caused bronchoconstriction in anaesthetized, mechanically ventilated guinea-pigs in the presence of propranolol (1 mg kg-1 i.v.). The geometric mean dose of BK required to produce 100% increase in airway opening pressure (PD100) was 22.9 nmol (95% c.i. 11.7-4...

journal_title：British journal of pharmacology

authors： Ichinose M,Barnes PJ

更新日期：1990-09-01 00:00:00