Novel roles for β-arrestins in the regulation of pharmacological sequestration to predict agonist-induced desensitization of dopamine D3 receptors.

abstract：:1 Morphine, Met-enkephalin, kyotorphin and D-phenylalanine have been applied by microiontophoresis to neurones in the globus pallidus and cerebral cortex of rats anaesthetized with urethane. 2 In the pallidum, most cells were inhibited by all the agonists, with a high correspondence between cells inhibited by Met-enke...

journal_title：British journal of pharmacology

authors： Stone TW

更新日期：1983-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The human kinome consists of roughly 500 kinases, including 150 that have been proposed as therapeutic targets. Protein kinases regulate an array of signalling pathways that control metabolism, cell cycle progression, cell death, differentiation and survival. It is not surprising, then, that new ...

journal_title：British journal of pharmacology

authors： Jensen BC,Parry TL,Huang W,Beak JY,Ilaiwy A,Bain JR,Newgard CB,Muehlbauer MJ,Patterson C,Johnson GL,Willis MS

更新日期：2017-12-01 00:00:00

abstract：:1. Experiments were performed in anaesthetized rabbits to examine the effects of calcitonin gene-related peptide (CGRP) and the CGRP antagonist CGRP8-37 on blood flow to the medial collateral ligament of the knee joint. 2. Topical application of CGRP (10(-13) to 10(-9) mol) to the exposed external surface of eight kne...

journal_title：British journal of pharmacology

authors： Ferrell WR,McDougall JJ,Bray RC

更新日期：1997-08-01 00:00:00

abstract：:1 Core and tail skin temperature was measured in rats which had guide cannulae implanted into their brains to allow drug injections directly into the preoptic anterior hypothalamus. 2 Apomorphine and dopamine (10 microgram in 1 microliter) injected into the area of the preoptic anterior hypothalamus caused a fall in c...

journal_title：British journal of pharmacology

authors： Cox B,Lee TF

更新日期：1977-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

journal_title：British journal of pharmacology

authors： Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

更新日期：2015-09-01 00:00:00

abstract：:1. Effects of KC399, an opener of ATP-sensitive K+ channels were investigated on membrane potential, isometric force and intracellular Ca2+ ([Ca2+]i) mobilization induced by acetylcholine (ACh) in smooth muscle from the rabbit trachea. 2. In these smooth muscle cells, ACh (0.1 and 1 microM) depolarized the membrane in...

journal_title：British journal of pharmacology

authors： Kamei K,Nabata H,Kuriyama H,Watanabe Y,Itoh T

更新日期：1995-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Diabetes is a risk factor for the development of coronary artery disease but it is not known whether the functions of endothelium-derived nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) in coronary arteries are altered in the early stage of diabetes. Such alterations and t...

journal_title：British journal of pharmacology

authors： Kajikuri J,Watanabe Y,Ito Y,Ito R,Yamamoto T,Itoh T

更新日期：2009-09-01 00:00:00

abstract：:1. Histamine and carbachol produced concentration-related increases in the accumulation of 3H-inositol phosphates in slices of bovine tracheal smooth muscle. 2. Noradrenaline alone produced a small stimulation of 3H-inositol phosphate accumulation which was inhibited by the alpha-adrenoceptor antagonist phentolamine. ...

journal_title：British journal of pharmacology

authors： Hall IP,Hill SJ

更新日期：1988-12-01 00:00:00

abstract：:1. beta-Bungarotoxin and other snake toxins with phospholipase activity augment acetylcholine release evoked from mouse motor nerve terminals before they produce blockade. This action of the toxins is independent of their phospholipase A2 activity, but the underlying mechanism for the facilitation of release is unclea...

journal_title：British journal of pharmacology

authors： Rowan EG,Harvey AL

更新日期：1988-07-01 00:00:00

abstract：:1. Use of the antihyperglycaemic agent, metformin, is often associated with a small rise in circulating lactate. This study investigates the source of the lactate and examines the effect of metformin on glucose metabolism by the intestine and liver of rats. 2. Changes in plasma glucose and lactate were measured in the...

journal_title：British journal of pharmacology

authors： Bailey CJ,Wilcock C,Day C

更新日期：1992-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:To determine whether there is an association between vascular NADPH oxidase (NOX), superoxide, the small GTPase Rac(1) and PDE type 5 (PDE5) in human vascular smooth muscle cell (hVSMCs). EXPERIMENTAL APPROACH:hVSMCs were incubated with xanthine-xanthine oxidase (X-XO; a superoxide generating sy...

journal_title：British journal of pharmacology

authors： Muzaffar S,Shukla N,Bond M,Sala-Newby GB,Newby AC,Angelini GD,Jeremy JY

更新日期：2008-11-01 00:00:00

abstract：:1. A method is presented which enables the dissociation constant (KI) of a competitive, pseudo-irreversible or non-competitive antagonist-receptor complex to be estimated without knowledge of agonist concentrations. 2. The technique has been tested using sets of concentration-response data which simulated these variou...

journal_title：British journal of pharmacology

authors： Mackay D

更新日期：1994-01-01 00:00:00

abstract：:1 The effect of clonidine on the 3H-purine release evoked by KCl or (-)-adrenaline was assessed in the superfused helical strip of the rabbit pulmonary artery pretreated with [3H]-adenosine. 2 Clonidine (3 x 10(-5) M to 10(-4) M) significantly enhanced the 3H-purine efflux evoked by 50 mM KCl but not by 3 x 10(-6) M) ...

journal_title：British journal of pharmacology

authors： Katsuragi T,Su C

更新日期：1981-11-01 00:00:00

abstract：:1. The ability of a range of substituted imidazole compounds to inhibit mouse cerebellar neuronal nitric oxide synthase (nNOS), bovine aortic endothelial NOS (eNOS) and inducible NOS (iNOS) from lungs of endotoxin-pretreated rats was investigated. In each case the substrate (L-arginine) concentration employed was 120 ...

journal_title：British journal of pharmacology

authors： Handy RL,Harb HL,Wallace P,Gaffen Z,Whitehead KJ,Moore PK

更新日期：1996-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Human lung fibroblasts (HLF) express high levels of the LPA1 receptor, a GPCR that responds to the endogenous lipid mediator, lysophosphatidic acid (LPA). Several molecular species or analogues of LPA exist and have been detected in biological fluids such as serum and plasma. The most widely expr...

journal_title：British journal of pharmacology

authors： Sattikar A,Dowling MR,Rosethorne EM

更新日期：2017-02-01 00:00:00

abstract：:1. Histamine contracted the tracheal and major bronchial muscles of sheep and relaxed the muscles of the lesser bronchi and bronchioles.2. The stimulant action of histamine on the trachea was antagonized by mepyramine, whereas the relaxant effect on the bronchial tree was not.3. 5-Hydroxytryptamine contracted the musc...

journal_title：British journal of pharmacology

authors： Yre P

更新日期：1969-07-01 00:00:00

abstract：:1. Recent studies demonstrated that inhibition or genetic inactivation of the enzyme poly (ADP-ribose) polymerase (PARP) is beneficial in myocardial reperfusion injury. PARP activation in the reperfused myocardium has been assumed, but not directly demonstrated. Furthermore, the issue whether pharmacological PARP inhi...

journal_title：British journal of pharmacology

authors： Liaudet L,Szabó E,Timashpolsky L,Virág L,Cziráki A,Szabó C

更新日期：2001-08-01 00:00:00

abstract：UNLABELLED:Reorganization of the actin cytoskeleton is essential for cell motility and chemotaxis. Actin-binding proteins (ABPs) and membrane lipids, especially phosphoinositides PI(4,5)P2 and PI(3,4,5)P3 are involved in the regulation of this reorganization. At least 15 ABPs have been reported to interact with, or reg...

journal_title：British journal of pharmacology

authors： Wu CY,Lin MW,Wu DC,Huang YB,Huang HT,Chen CL

更新日期：2014-12-01 00:00:00

abstract：:1. Inflammatory diseases of the pancreas or diseases which cause obstruction within the biliary or within the biliary or pancreatic duct system are associated with severe pain. Although neuropeptides such as substance P are present in the biliary tree, only few capsaicin-sensitive, substance P-positive nerve fibres ha...

journal_title：British journal of pharmacology

authors： Griesbacher T

更新日期：1994-02-01 00:00:00

abstract：UNLABELLED:Sarcoplasmic reticular (SR) Ca(2+) -ATPase (SERCA2a) is central to cardiac electrophysiological and mechanical function. It ensures full diastolic relaxation minimizing delayed after-potentials that would otherwise compromise membrane electrophysiological stability, and optimizes SR Ca(2+) refilling and syst...

journal_title：British journal of pharmacology

authors： Huang CL

更新日期：2013-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The anti-cancer agent [Arg(6), D-Trp(7,9), N(me)Phe(8)]-substance P (6-11) (SP-G) modulates gastrin releasing peptide (GRP) and arginine vasopressin signalling in small cell lung cancer cells leading to growth arrest and apoptosis. We have shown that SP-G acts as a biased agonist at GRP receptors...

journal_title：British journal of pharmacology

authors： MacKinnon AC,Tufail-Hanif U,Wheatley M,Rossi AG,Haslett C,Seckl M,Sethi T

更新日期：2009-01-01 00:00:00

abstract：:Halothane has many effects on the resting membrane potential (V(m)) of excitable cells and exerts numerous effects on skeletal muscle one of which is the enhancement of Ca(2+) release by the sarcoplasmic reticulum (SR) resulting in a sustained contracture. The aim of this study was to analyse the effects of clinical d...

journal_title：British journal of pharmacology

authors： Sauviat MP,Frizelle HP,Descorps-Declère A,Mazoit JX

更新日期：2000-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Early soluble epoxide hydrolase inhibitors (sEHIs) such as 12-(3-adamantan-1-yl-ureido)-dodecanoic acid (AUDA) are effective anti-hypertensive and anti-inflammatory agents in various animal models. However, their poor metabolic stability and limited water solubility make them difficult to use pha...

journal_title：British journal of pharmacology

authors： Liu JY,Tsai HJ,Hwang SH,Jones PD,Morisseau C,Hammock BD

更新日期：2009-01-01 00:00:00

abstract：:1. 5-HT and the prostanoid TP receptor agonists, U46619 and I-BOP, constricted the human umbilical artery with pEC50 values of 7.3+/-0. 2, 6.7+/-0.1, and 7.3+/-0.2, respectively. The selective TP receptor antagonist, GR32191 (0.1 microM), shifted the concentration-effect curves to U46619 and I-BOP to the right, but ha...

journal_title：British journal of pharmacology

authors： Boersma JI,Janzen KM,Oliveira L,Crankshaw DJ

更新日期：1999-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Voltage-gated sodium channels (VGSCs) are assembled from two classes of subunits, a pore-bearing α-subunit (NaV 1) and one or two accessory β-subunits (NaV βs). Neurons in mammals can express one or more of seven isoforms of NaV 1 and one or more of four isoforms of NaV β. The peptide μ-conotoxin...

journal_title：British journal of pharmacology

authors： Zhang MM,Wilson MJ,Azam L,Gajewiak J,Rivier JE,Bulaj G,Olivera BM,Yoshikami D

更新日期：2013-04-01 00:00:00

abstract：:Rabbits treated with 2-deoxy-D-glucose (2DG) (300 mg/kg) show an increased intake of food and water. Pretreatment with haloperidol (1 mg/kg) abolishes the increase in water intake but does not prevent the increase in food intake. ...

journal_title：British journal of pharmacology

authors： Anderson J,Sharman DF,Stephens DB

更新日期：1979-05-01 00:00:00

abstract：:1. Block by philanthotoxin-343 (PhTX-343), a neurotoxin from wasps, of ionic currents mediated through neuronal nicotinic acetylcholine (ACh) receptor/channels was characterized in rat phaeochromocytoma PC12 cells, by use of whole cell voltage-clamp techniques. 2. In the cells held at -60 mV, PhTX-343 at 0.1 and 1 mic...

journal_title：British journal of pharmacology

authors： Liu M,Nakazawa K,Inoue K,Ohno Y

更新日期：1997-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Some neurosteroids, notably 3alpha-hydroxysteroids, positively modulate GABA(A) receptors, but sulphated steroids negatively modulate these receptors. Recently, other lipophilic amphiphiles have been suggested to positively modulate GABA receptors. We examined whether there was similarity among t...

journal_title：British journal of pharmacology

authors： Chisari M,Shu HJ,Taylor A,Steinbach JH,Zorumski CF,Mennerick S

更新日期：2010-05-01 00:00:00

abstract：:1. Endothelial cells, under given circumstances, can initiate contraction (constriction) of the vascular smooth muscle cells that surround them. Such endothelium-dependent, acute increases in contractile tone can be due to the withdrawal of the production of nitric oxide, to the production of vasoconstrictor peptides ...

journal_title：British journal of pharmacology

authors： Vanhoutte PM,Feletou M,Taddei S

更新日期：2005-02-01 00:00:00

abstract：:The effect of activation of protein kinase C (PKC) or adenylyl cyclase on release of glutamate has been investigated in a perfused slice preparation from the rat caudal trigeminal nucleus. Stimulation of PKC by phorbol 12-myristate 13-acetate (PMA) produced a concentration-dependent increase in K(+)-evoked release of ...

journal_title：British journal of pharmacology

authors： Maneuf YP,McKnight AT

更新日期：2001-09-01 00:00:00