The GABAβ receptor as a target for antidepressant drug action.

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：:A new C5a receptor antagonist, the cyclic peptide Phe-[Orn-Pro-D-cyclohexylalanine-Trp-Arg], (F-[OPdChaWR]), was tested for its ability to antagonize the neutropenic effects of both C5a and endotoxin in rats. Human recombinant C5a (2 microg kg(-1) i.v.) caused rapid neutropenia, characterized by an 83% decrease in cir...

journal_title：British journal of pharmacology

authors： Short A,Wong AK,Finch AM,Haaima G,Shiels IA,Fairlie DP,Taylor SM

更新日期：1999-02-01 00:00:00

abstract：:1. In the present study the effect of N-methyl-D-aspartate (NMDA) on thromboxane B2 synthesis and on [Ca2+]i was studied in human platelets. 2. NMDA (10(-7) M) completely inhibited the synthesis of thromboxane B2 from exogenous arachidonic acid (AA), while it did not interfere with the aggregating effect of the thromb...

journal_title：British journal of pharmacology

authors： Franconi F,Miceli M,Alberti L,Seghieri G,De Montis MG,Tagliamonte A

更新日期：1998-05-01 00:00:00

abstract：:1. Pre-eclampsia is a serious pregnancy disorder associated with widespread activation of the maternal vascular endothelium. Recent evidence implicates a role for oxidative stress in the aetiology of this condition. 2. Reactive oxygen species, particularly superoxide anions, invokes endothelial cell activation through...

journal_title：British journal of pharmacology

authors： Crocker IP,Kenny LC,Thornton WA,Szabo C,Baker PN

更新日期：2005-03-01 00:00:00

abstract：:1 The binding of [3H]-muscimol, a potent gamma-aminobutyric acid (GABA) receptor agonist, to crude membrane preparations of bovine retina was studied, using a filtration method to isolate membrane-bound ligand. 2 Specific binding was found to be saturable and occurred at two binding sites with affinity constants of 4....

journal_title：British journal of pharmacology

authors： Osborne NN

更新日期：1980-01-01 00:00:00

abstract：:Research into the pharmacology of individual cannabinoids that began in the 1940s, several decades after the presence of a cannabinoid was first detected in cannabis, is concisely reviewed. Also described is how this pharmacological research led to the discovery of cannabinoid CB(1) and CB(2) receptors and of endogeno...

journal_title：British journal of pharmacology

authors： Pertwee RG

更新日期：2006-01-01 00:00:00

abstract：:1 Physiologically, perisinusoidal hepatic stellate cells (HSC) are quiescent and store retinoids. During liver injury and in cell culture, HSC transform into proliferating myofibroblast-like cells that express alpha-smooth muscle actin (alpha-sma) and produce excessive amounts of extracellular matrix. During transform...

journal_title：British journal of pharmacology

authors： Chi X,Anselmi K,Watkins S,Gandhi CR

更新日期：2003-06-01 00:00:00

abstract：:1. Superoxide dismutase (SOD, 60 u ml-1) or ferricytochrome c (70 microM) significantly inhibited thrombin-stimulated platelet adhesion to gelatin-coated plastic, whereas catalase (1000 u ml-1) or mannitol (1 mM) had no effect. 2. The platelet aggregation induced by low concentrations of thrombin (causing less than 45...

journal_title：British journal of pharmacology

authors： Salvemini D,de Nucci G,Sneddon JM,Vane JR

更新日期：1989-08-01 00:00:00

abstract：:1. Column chromatography with Agarose A50m followed by Sephadex G100 was used to separate a fraction (extract II) in the molecular weight range 12,000 to 14,000 daltons from saline extracts of the sea anemone, Tealia felina. 2. Extract II inhibited histamine-induced contractions of the guinea-pig ileum and produced ha...

journal_title：British journal of pharmacology

authors： Aldeen SI,Elliott RC,Sheardown M

更新日期：1981-02-01 00:00:00

abstract：:1. Intracellular recordings were made from neurones in vitro in the rat substantia nigra zona compacta and ventral tegmental area; the neurones had the characteristic properties of dopamine-containing cells, and fired action potentials spontaneously. 2. Cocaine (1-10 microM) inhibited spontaneous firing, hyperpolarize...

journal_title：British journal of pharmacology

authors： Lacey MG,Mercuri NB,North RA

更新日期：1990-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The human prostacyclin receptor (hIP), a G-protein coupled receptor (GPCR) expressed mainly on platelets and vascular smooth muscle cells, plays important protective roles in the cardiovascular system. We hypothesized that significant insights could be gained into the structure and function of th...

journal_title：British journal of pharmacology

authors： Stitham J,Arehart E,Gleim SR,Li N,Douville K,Hwa J

更新日期：2007-10-01 00:00:00

abstract：:5-Lipoxygenase (5-LO) is a crucial enzyme in the synthesis of the bioactive leukotrienes (LTs) from arachidonic acid (AA), and inhibitors of 5-LO are thought to prevent the untowarded pathophysiological effects of LTs. In this study, we present the molecular pharmacological profile of the novel nonredox-type 5-LO inhi...

journal_title：British journal of pharmacology

authors： Fischer L,Steinhilber D,Werz O

更新日期：2004-07-01 00:00:00

abstract：:1. Male, Long Evans rats were instrumented chronically with pulsed Doppler probes and intravascular catheters to allow assessment of regional haemodynamic changes during i.v. infusion of lipopolysaccharide (LPS, 150 micrograms kg-1 h-1). 2. In the presence of the AT1-receptor antagonists, losartan (10 mg kg-1 + 10 kg-...

journal_title：British journal of pharmacology

authors： Gardiner SM,Kemp PA,March JE,Bennett T

更新日期：1996-12-01 00:00:00

abstract：:1 Synaptic potentials and the responses of frog spinal cord to various acidic amino acids were examined by means of the sucrose gap recording technique. 2 Divalent cations (50-250 microM) specifically antagonized responses evoked at N-methyl-D-aspartate (NMDA) receptors by N-methyl D,L aspartic acid (NMDLA). The rank ...

journal_title：British journal of pharmacology

authors： Smith PA

更新日期：1982-10-01 00:00:00

abstract：:1. Ca currents in rat and mouse sensory dorsal root ganglion (DRG) neurones were inhibited by concentrations of (-)-baclofen as low as 1 micron. The proportion of neurones responding to baclofen was low (less than 20%), except in young cultures of neonate rat DRG neurones (3 days in culture), where 86% of the neurones...

journal_title：British journal of pharmacology

authors： Green KA,Cottrell GA

更新日期：1988-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The effects of bergamot essential oil (BEO; Citrus bergamia, Risso) on excitotoxic neuronal damage was investigated in vitro. EXPERIMENTAL APPROACH:The study was performed in human SH-SY5Y neuroblastoma cells exposed to N-methyl-D-aspartate (NMDA). Cell viability was measured by dye exclusion. R...

journal_title：British journal of pharmacology

authors： Corasaniti MT,Maiuolo J,Maida S,Fratto V,Navarra M,Russo R,Amantea D,Morrone LA,Bagetta G

更新日期：2007-06-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an adult-onset neurodegenerative disease characterized by the selective death of upper and lower motor neurons which ultimately leads to paralysis and ultimately death. Pathological changes in ALS are closely associated with pronounced and progressive changes in mitochondrial mor...

journal_title：British journal of pharmacology

authors： Muyderman H,Chen T

更新日期：2014-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:MLN4924 prevents the formation of active cullin-RING ubiquitin ligase complexes and thus inhibits NF-κB signalling. Here, we evaluated the effects of this compound on monocytes and dendritic cells (DCs). EXPERIMENTAL APPROACH:Monocytes and DCs were challenged with TNF or LPS in the presence and ...

journal_title：British journal of pharmacology

authors： El-Mesery M,Seher A,Stühmer T,Siegmund D,Wajant H

更新日期：2015-03-01 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. Electrically-evoked contractions in different regions of the rabbit isolated pulmonary artery have been investigated using stimulation parameters generally assumed to stimulate nerves selectively. 2. In extrapulmonary artery, trains of stimuli (10 Hz; pulse width 0.1 ms) evoked monophasic contractions. In contrast,...

journal_title：British journal of pharmacology

authors： Jackson VM,Trout SJ,Cunnane TC

更新日期：2002-10-01 00:00:00

abstract：:1 A series of cationic, lipophilic histamine H1-receptor antagonists, neuroleptics, antidepressants and monoamine oxidase inhibitors were tested for their effects on anti-IgE-induced histamine release from human lung fragments in vitro. 2 They had a biphasic effect: at low concentrations a dose-related inhibition of h...

journal_title：British journal of pharmacology

authors： Church MK,Gradidge CF

更新日期：1980-08-01 00:00:00

abstract：:1. The release of prostaglandin D2 (PGD2) during immediate allergic reactions in human skin was investigated in vivo and in vitro. 2. Skin exudates were collected from abraded sites on the thigh of atopic subjects sensitive to D. pteronyssinus antigen and from non-atopic control subjects. Challenge with antigen caused...

journal_title：British journal of pharmacology

authors： Barr RM,Koro O,Francis DM,Black AK,Numata T,Greaves MW

更新日期：1988-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tooth eruption is a complicated process regulated by the dental follicles (DF). Our recent study discovered that tooth eruption was inhibited upon injection of bleomycin into DF. However, the mechanisms were unknown. EXPERIMENTAL APPROACH:Human dental follicle cells (hDFCs) were treated by bleom...

journal_title：British journal of pharmacology

authors： Li ZZ,Wang HT,Lee GY,Yang Y,Zou YP,Wang B,Gong CJ,Cai Y,Ren JG,Zhao JH

更新日期：2020-10-17 00:00:00

abstract：:1 Contractions of the cat nictitating membrane were elicited on stimulation of the internal carotid nerve, and the effects were studied of desipramine and two inhibitors of catechol-O-methyltransferase, U-0521 and pyrogallol, on the subsequent relaxation of the muscle. 2 The relaxation of the nictitating membrane occu...

journal_title：British journal of pharmacology

authors： Eccles R,Maclean AG

更新日期：1978-04-01 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：:Ligands targeting GPCRs can be categorized according to their intrinsic efficacy to trigger a specific, receptor-mediated response. A ligand endowed with the same level of efficacy as the endogenous agonist can be classified as a full agonist, whereas a compound that displays greater efficacy, that is, higher receptor...

journal_title：British journal of pharmacology

authors： Schrage R,De Min A,Hochheiser K,Kostenis E,Mohr K

更新日期：2016-10-01 00:00:00

abstract：:1 The rates at which tubocurarine associates with, and dissociates from, the nicotinic receptor, while exerting its classical competitive effect, are still in doubt. We have investigated this problem by observing the effect of low concentrations of tubocurarine on the re-equilibration rate, following a step change in ...

journal_title：British journal of pharmacology

authors： Colquhoun D,Sheridan RE

更新日期：1982-01-01 00:00:00

abstract：:1 N-2-Chlorethyl-N-ethyl-2-bromobenzylamine hydrochloride (DSP 4) 50 mg/kg intraperitoneally, produced a long-term decrease in the capacity of brain homogenates to accumulate noradrenaline with significant effect 8 months after the injection. It had no effect on the noradrenaline uptake in homogenates from the striatu...

journal_title：British journal of pharmacology

authors： Ross SB

更新日期：1976-12-01 00:00:00

abstract：BACKGROUND:5-HT(2B) receptors are localized within the myenteric nervous system, but their functions on motor/sensory neurons are unclear. To explore the role of these receptors, we further characterized the 5-HT(2B) receptor antagonist RS-127445 and studied its effects on peristalsis and defecation. EXPERIMENTAL APPR...

journal_title：British journal of pharmacology

authors： Bassil AK,Taylor CM,Bolton VJ,Gray KM,Brown JD,Cutler L,Summerfield SG,Bruton G,Winchester WJ,Lee K,Sanger GJ

更新日期：2009-09-01 00:00:00

abstract：:1 The effect of compound 48/80 was studied on the twitch-like contractions of the longitudinal muscle of guinea-pig ileum induced by electrical stimulation of intramural cholinergic nerves. 2 Compound 48/80 alone, at concentrations up to 30 microgram/ml, had no effect on the twitch contractions. The contraction to exo...

journal_title：British journal of pharmacology

authors： Kamikawa Y,Shimo Y

更新日期：1978-12-01 00:00:00