Effects of cholecystokinin and related peptides on neuronal activity in the ventromedial nucleus of the rat hypothalamus.

abstract：:The human distal gut is home to a rich and dense microbial community with representatives of all three domains of life which are intricately connected with our physiology and health. The combined genomes of these microbes, collectively called the human microbiome, vastly expand the metabolic capacities of our own geno...

journal_title：British journal of pharmacology

authors： Bik EM,Ugalde JA,Cousins J,Goddard AD,Richman J,Apte ZS

更新日期：2018-12-01 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：:Melatonin receptors are seven transmembrane-spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist - MT1 and MT2 - encoded by the MTNR1A and MTNR1B genes respectively. The current review provides an update on melatonin receptors by the corresponding subcommittee of the I...

journal_title：British journal of pharmacology

authors： Jockers R,Delagrange P,Dubocovich ML,Markus RP,Renault N,Tosini G,Cecon E,Zlotos DP

更新日期：2016-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Evidence suggests that exercise decreases nicotine withdrawal symptoms in humans; however, the mechanisms mediating this effect are unclear. We investigated, in a mouse model, the effect of exercise intensity during chronic nicotine exposure on nicotine withdrawal severity, binding of α4β2*, α7 n...

journal_title：British journal of pharmacology

authors： Keyworth H,Georgiou P,Zanos P,Rueda AV,Chen Y,Kitchen I,Camarini R,Cropley M,Bailey A

更新日期：2018-06-01 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：:1. In the present study we tested the hypothesis that insulin-like growth factor-1 (IGF-1) modulates resting chloride conductance (G(Cl)) of rat skeletal muscle by activating a phosphatase and that the chloride channel, based on the activity of phosphorylating-dephosphorylating pathways, has different sensitivity to s...

journal_title：British journal of pharmacology

authors： De Luca A,Pierno S,Liantonio A,Camerino C,Conte Camerino D

更新日期：1998-10-01 00:00:00

abstract：:1. The sinus node inhibitors UL FS 49 and DK-AH 269 reduce heart rate by slowing diastolic depolarization rate in the sino-atrial (SA) node, which might originate from the use-dependent blockade of a hyperpolarization-activated current If. A hyperpolarization-activated current Ih, which is present in many types of neu...

journal_title：British journal of pharmacology

authors： Raes A,Van de Vijver G,Goethals M,van Bogaert PP

更新日期：1998-10-01 00:00:00

abstract：:1. Riluzole has been shown to have beneficial effects in motoneurone disease, yet its effect on motoneurones is not known. To address this question, we investigated synaptic modulation by riluzole in hypoglossal motoneurones by recording glycinergic inhibitory postsynaptic currents evoked by stimulation of nearby sing...

journal_title：British journal of pharmacology

authors： Umemiya M,Berger AJ

更新日期：1995-12-01 00:00:00

abstract：:1. Pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS), a P2-purinoceptor antagonist, was investigated for its ability to antagonize: (1) P2X-purinoceptor-mediated contractions of the rabbit central ear artery and saphenous artery evoked by either alpha,beta-methylene ATP (alpha,beta-MeATP) or electrical fie...

journal_title：British journal of pharmacology

authors： Ziganshin AU,Hoyle CH,Lambrecht G,Mutschler E,Bümert HG,Burnstock G

更新日期：1994-03-01 00:00:00

abstract：:The effects of adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), and adenosine on compound action potentials were investigated in de-sheathed frog-sciatic nerve preparations. ATP and ADP but not adenosine antagonized the inhibitory action of tetrodotoxin (TTX) on nerve conductio...

journal_title：British journal of pharmacology

authors： Ribeiro JA,Sebastião AM

更新日期：1984-02-01 00:00:00

abstract：:After many years of effort, recent technical breakthroughs have enabled the X-ray crystal structures of three G-protein-coupled receptors (GPCRs) (beta1 and beta2 adrenergic and adenosine A(2a)) to be solved in addition to rhodopsin. GPCRs, like other membrane proteins, have lagged behind soluble drug targets such as ...

journal_title：British journal of pharmacology

authors： Congreve M,Marshall F

更新日期：2010-03-01 00:00:00

abstract：:1. Microinjection of peptide YY (PYY, 7-46 pmol) into the dorsal vagal complex (DVC) stimulated gastric acid secretion in urethane-anaesthetized rats. Using a variety of neuropeptide Y (NPY) and PYY derivatives, we characterized the pharmacological profile of the receptor mediating the acid secretory response to PYY. ...

journal_title：British journal of pharmacology

authors： Yang H,Li WP,Reeve JR Jr,Rivier J,Taché Y

更新日期：1998-04-01 00:00:00

abstract：:1. The effects of the selective alpha 2-adrenoceptor agonist, medetomidine, were assessed on plasma levels of immunoreactive atrial natriuretic peptide (IR-ANP), haemodynamics and on urine water and solute excretion in conscious, chronically cannulated, 7 month-old spontaneously hypertensive (SHR) and age-matched Wist...

journal_title：British journal of pharmacology

authors： Ruskoaho H,Leppäluoto J

更新日期：1989-05-01 00:00:00

abstract：:The gastrointestinal (GI) tract is exposed to a large array of proteases, under both physiological and pathophysiological conditions. The discovery of G protein-coupled receptors activated by proteases, the protease-activated receptors (PARs), has highlighted new signaling functions for proteases in the GI tract, part...

journal_title：British journal of pharmacology

authors： Vergnolle N

更新日期：2004-04-01 00:00:00

abstract：:1. This study sets out to examine the effect of rilmenidine administered systemically on basal and reflexly activated renal nerve activity in Wistar and stroke prone spontaneously hypertensive rats (SHRSP). 2. Animals were anaesthetized with chloralose/urethane, stimulating electrodes were placed on the brachial plexi...

journal_title：British journal of pharmacology

authors： Zhang T,Johns EJ

更新日期：1996-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:alpha5IA (3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine) is a triazolophthalazine with subnanomolar affinity for alpha1-, alpha2-, alpha3- and alpha5-containing GABA(A) receptors. Here we have evaluated the relationship between plasma alpha5...

journal_title：British journal of pharmacology

authors： Atack JR,Eng WS,Gibson RE,Ryan C,Francis B,Sohal B,Dawson GR,Hargreaves RJ,Burns HD

更新日期：2009-07-01 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：BACKGROUND AND PURPOSE:The use of tubulin-binding compounds, which act in part by inhibiting tumour angiogenesis, has become an integral strategy of tumour therapy. Recently, tubulysins were identified as a novel class of natural compounds of myxobacterial origin, which inhibit tubulin polymerization. As these compound...

journal_title：British journal of pharmacology

authors： Rath S,Liebl J,Fürst R,Ullrich A,Burkhart JL,Kazmaier U,Herrmann J,Müller R,Günther M,Schreiner L,Wagner E,Vollmar AM,Zahler S

更新日期：2012-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Thromboxane A(2) and endothelial dysfunction are implicated in the development of pulmonary hypertension. The receptor-transduction pathway for U46619 (9,11-dideoxy-9 alpha, 11 alpha-methanoepoxy prostaglandin F(2 alpha))-induced contraction was examined in endothelium-intact (E+) and denuded (E-...

journal_title：British journal of pharmacology

authors： McKenzie C,MacDonald A,Shaw AM

更新日期：2009-06-01 00:00:00

abstract：:N-ethylmaleimide (NEM) has been reported to interact with the GTP-binding Ni-protein; we have examined its effect on adenosine receptor binding in feline cortical membranes and on adenosine-receptor mediated effects on cyclic AMP accumulation in rat hippocampal slices. Treatment of cortical membranes with NEM (100 mic...

journal_title：British journal of pharmacology

authors： Fredholm BB,Lindgren E,Lindström K

更新日期：1985-10-01 00:00:00

abstract：:1. An 'atypical' 5-HT2 receptor which is located on the endothelium of rat jugular vein has been described. In the present study we have further defined the nature of the 5-HT2 receptor subtype present in this preparation. 2. In experiments conducted in the presence of ketanserin to preclude involvement of 5-HT2 recep...

journal_title：British journal of pharmacology

authors： Ellis ES,Byrne C,Murphy OE,Tilford NS,Baxter GS

更新日期：1995-01-01 00:00:00

abstract：:N-terminal labelled fluorescent BODIPY-NPY peptide analogues were tested in Y1, Y2, Y4 and Y5 receptor-binding assays performed in rat brain membrane preparations and HEK293 cells expressing the rat Y1, Y2, Y4 and Y5 receptors. BODIPY TMR/FL-[Leu31, Pro34]NPY/PYY were able to compete for specific [125][Leu31, Pro34]PY...

journal_title：British journal of pharmacology

authors： Dumont Y,Gaudreau P,Mazzuferi M,Langlois D,Chabot JG,Fournier A,Simonato M,Quirion R

更新日期：2005-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Proteinase activated receptor 2 (PAR2) is a GPCR associated with inflammation, metabolism and disease. Clues to understanding how to block PAR2 signalling associated with disease without inhibiting PAR2 activation in normal physiology could be provided by studies of biased signalling. EXPERIMENT...

journal_title：British journal of pharmacology

authors： Suen JY,Cotterell A,Lohman RJ,Lim J,Han A,Yau MK,Liu L,Cooper MA,Vesey DA,Fairlie DP

更新日期：2014-09-01 00:00:00

abstract：:1. Non-steroidal anti-inflammatory drugs (NSAIDs) are effective anti-inflammatory and analgesic drugs although they also induce unwanted side effects due to the inhibition of the physiological effects regulated by prostaglandins. This has led to the search for new compounds with fewer side effects, such as the nitro-N...

journal_title：British journal of pharmacology

authors： Romero-Sandoval EA,Mazario J,Howat D,Herrero JF

更新日期：2002-03-01 00:00:00

abstract：:1. Endothelin, a novel potent vasoconstrictor peptide produced by vascular endothelial cells stimulated anion secretion by a cultured secretory epithelium derived from the rat epididymis as measured by changes in short-circuit current (SCC). 2. Stimulation of the SCC was observed when endothelin was added to the basol...

journal_title：British journal of pharmacology

authors： Wong PY,Fu WO,Huang SJ

更新日期：1989-12-01 00:00:00

abstract：:Chemotherapy-induced immune-suppression is a common, but potential detrimental, adverse reaction in patients undergoing treatment for cancer and strategies with capacity to boost the immune cell populations are needed. Physical exercise training is a potent regulator of immune cell viability and function and may serve...

journal_title：British journal of pharmacology

authors： Schauer T,Hojman P,Gehl J,Christensen JF

更新日期：2020-05-25 00:00:00

abstract：:1. Tyrosine kinases have been proposed as regulators of voltage-operated calcium channels. The effects of a range of structurally different inhibitors of protein tyrosine kinases (PTK) were examined on voltage-operated calcium channel currents (I(Ba)) and pp60(c-src) kinase (c-src) activity in vitro. 2. I(Ba) was meas...

journal_title：British journal of pharmacology

authors： Wijetunge S,Lymn JS,Hughes AD

更新日期：2000-04-01 00:00:00

abstract：:1. Taxanes are antineoplastic drugs which have cardiovascular side effects of unknown mechanism. We investigated their influence on blood viscosity and erythrocyte morphology. 2. Whole blood was incubated in vitro with increasing concentrations of Taxol, Taxotere, paclitaxel (0-100 microM) and the vehicles Cremophor-E...

journal_title：British journal of pharmacology

authors： Mark M,Walter R,Meredith DO,Reinhart WH

更新日期：2001-11-01 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. We investigated the mechanism of action of two novel nonsulphonylurea ATP-sensitive potassium channel (K(ATP)) inhibitors, PNU-99963 and PNU-37883A, on four types of cloned K(ATP) channels. 2. Whole-cell currents were recorded in a symmetrical potassium (140 mM) gradient in HEK-293 cells stably expressing Kir6.2/SU...

journal_title：British journal of pharmacology

authors： Cui Y,Tinker A,Clapp LH

更新日期：2003-05-01 00:00:00