Recent progress in the understanding of relaxin family peptides and their receptors.

abstract：:1 The recently discovered benzodiazepine receptor exists in high concentration in the cerebral cortex. We have, therefore, examined the effects of diazepam and chlordiazepoxide on cortical neurone responses to excitatory and inhibitory amino acids and acetylcholine, in the cortex of rats anaesthetized with urethane.2 ...

journal_title：British journal of pharmacology

authors： Assumpção JA,Bernardi N,Brown J,Stone TW

更新日期：1979-12-01 00:00:00

abstract：:1. The putative alpha 1-adrenoceptor subtypes of rat cerebral cortex membranes were characterized in binding. 2. Specific binding of [3H]-prazosin was saturable between 20-5000 pm. Scatchard plots of the binding data were non-linear, indicating the presence of two distinct affinity sites for prazosin (pKD, high = 10.1...

journal_title：British journal of pharmacology

authors： Oshita M,Kigoshi S,Muramatsu I

更新日期：1991-12-01 00:00:00

abstract：:The modulation of the gamma-aminobutyric acidA (GABAA) receptor by alphaxalone has been investigated by use of voltage-clamp recordings from enzymatically isolated bovine chromaffin cells maintained in cell culture. Alphaxalone (greater than 30 nM) reversibly and dose-dependently potentiated the amplitude of membrane ...

journal_title：British journal of pharmacology

authors： Cottrell GA,Lambert JJ,Peters JA

更新日期：1987-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Aminoguanidine (AG), an inhibitor of advanced glycation endproducts, has been shown to prevent arterial stiffening and cardiac hypertrophy in streptozotocin (STZ) and nicotinamide (NA)-induced type 2 diabetes in rats. Our aims were to examine whether AG produced benefits on cardiac pumping mechan...

journal_title：British journal of pharmacology

authors： Wu MS,Liang JT,Lin YD,Wu ET,Tseng YZ,Chang KC

更新日期：2008-06-01 00:00:00

abstract：:We compared the modulation of synaptic transmission by adenosine A(1) receptors in the hippocampus of aged (24 months) and young adult rats (6 weeks). The adenosine A(1) receptor agonist, N(6)-cyclopentyladenosine, was less potent (P:<0.05) to inhibit synaptic transmission in aged (EC(50)=53 nM) than young adult (EC(5...

journal_title：British journal of pharmacology

authors： Sebastião AM,Cunha RA,de Mendonça A,Ribeiro JA

更新日期：2000-12-01 00:00:00

abstract：:1. Rat mesenteric (approximately 250 microns) were set up in a single-channel isometric myograph designed to allow with 6 microM fura-2AM for 2 h and simultaneous recordings of neurogenic contraction (force) and intracellular calcium [Ca2+]i were obtained. In other experiments, arteries were loaded with 1 microCi ml-1...

journal_title：British journal of pharmacology

authors： Garcha RS,Hughes AD

更新日期：1997-09-01 00:00:00

abstract：:1. Losigamone is a novel anticonvulsant the mechanism of action of which is not known. This study investigated the effect of losigamone on spontaneous, NMDA- and AMPA-induced depolarizations in the cortical wedge preparation of the DBA/2 mouse (which are susceptible to sound-induced seizures) and on endogenous amino a...

journal_title：British journal of pharmacology

authors： Srinivasan J,Richens A,Davies JA

更新日期：1997-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Emesis is a multi-system reflex, which is usually investigated using in vivo models. The aim of the study is to compare the response induced by emetic compounds across species and investigate whether dogs, ferrets and rats are all similarly predictive of humans. EXPERIMENTAL APPROACH:A systemati...

journal_title：British journal of pharmacology

authors： du Sert NP,Holmes AM,Wallis R,Andrews PL

更新日期：2012-03-01 00:00:00

abstract：:1. Conscious, Long Evans rats (n = 10), chronically instrumented for the measurement of regional haemodynamics, were studied on 3 consecutive experimental days to assess responses to angiotensin II (AII) (125 pmol kg-1, i.v.) and noradrenaline (1 nmol kg-1, i.v.) in the absence and presence of the AT2-receptor antagon...

journal_title：British journal of pharmacology

authors： Widdop RE,Gardiner SM,Kemp PA,Bennett T

更新日期：1992-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Strontium ranelate reduces fracture risk in postmenopausal women with osteoporosis. Evidence from non-clinical studies and analyses of bone markers in phase III trials indicate that this is due to an increase in osteoblast formation and a decrease of osteoclastic resorption. The aim of this work ...

journal_title：British journal of pharmacology

authors： Brennan TC,Rybchyn MS,Green W,Atwa S,Conigrave AD,Mason RS

更新日期：2009-08-01 00:00:00

abstract：:1. The effect of the nootropic drug, piracetam on stress- and subsequent morphine-induced prolactin (PRL) secretion was investigated in vivo in male rats, by use of a stress-free blood sampling and drug administration method by means of a permanent indwelling catheter in the right jugular vein. 2. Four doses of pirace...

journal_title：British journal of pharmacology

authors： Matton A,Engelborghs S,Bollengier F,Finné E,Vanhaeist L

更新日期：1996-02-01 00:00:00

abstract：:Initiation of 60 min ischaemia to rat isolated hearts produced a depression in developed tension and heart rate. Subsequent reperfusion caused a greatly exacerbated creatine phosphokinase (CPK) efflux and limited functional recovery. Sulphinpyrazone (100 ng ml-1 and 1 microgram ml-1) significantly reduced CPK release,...

journal_title：British journal of pharmacology

authors： Karmazyn M

更新日期：1984-09-01 00:00:00

abstract：:1 Poly (ADP-ribose) synthetase (PARS) is a nuclear enzyme activated by strand breaks in DNA, which are caused by reactive oxygen species (ROS). Here we investigate the effects of the PARS inhibitors 3-aminobenzamide (3-AB), nicotinamide and 1,5-dihydroxyisoquinoline (ISO) on the circulatory failure and the organ injur...

journal_title：British journal of pharmacology

authors： McDonald MC,Filipe HM,Thiemermann C

更新日期：1999-11-01 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. We previously showed that chronic exposure to aspirin (100 mg kg-1 daily, by mouth) is effective in preventing the onset of hypertension in young (28-84 day old) spontaneously hypertensive rats (SHRs). This is contrary to what others have reported using older SHRs. 2. Renal prostaglandin F2 alpha was also reduced i...

journal_title：British journal of pharmacology

authors： Tuttle RS,Yager J,Northrup N

更新日期：1988-07-01 00:00:00

abstract：:5-Hydroxytryptamine (5-HT) evoked potent contractile responses in phenoxybenzamine-treated ring segments of rat caudal artery, partially contracted with U46619. Responses were mimicked by 5-HT1-selective agonists with the potency order: RU24969 > 5-carboxamidotryptamine > 5-HT = CP-93,129 > sumatriptan. 8-Hydroxy-N,N-...

journal_title：British journal of pharmacology

authors： Craig DA,Martin GR

更新日期：1993-07-01 00:00:00

abstract：:We have examined the effects of antagonists on the isometric contraction of the human saphenous vein produced by 5-hydroxytryptamine (5-HT). The 5-HT2-antagonist ketanserin (1 microM) had little effect on the lower part of the concentration-response curve to 5-HT, but markedly shifted the upper part of the curve. Yohi...

journal_title：British journal of pharmacology

authors： Docherty JR,Hyland L

更新日期：1986-09-01 00:00:00

abstract：:1. The uptake of (3)H-digitoxin, (3)H-ouabain and (3)H-dihydro-ouabain by isolated guinea-pig atria has been studied and compared with the inhibition of the sodium pump and with the inotropic effect.2. Analysis of the curve relating the uptake of digitoxin and ouabain at equilibrium to the bath concentration enabled a...

journal_title：British journal of pharmacology

authors： Godfraind T,Lesne M

更新日期：1972-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Deletion of the cyclooxygenase-2 (COX-2) gene causes impairment of kidney development, but the effect of selective inhibitors of COX-2 (coxibs) or the non-selective inhibitors of COX (the classical non-steroidal anti-inflammatory drugs; NSAIDs) on kidney development was less well described. EXPE...

journal_title：British journal of pharmacology

authors： Olliges A,Wimmer S,Nüsing RM

更新日期：2011-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT (serotonin) regulates various physiological functions, both directly and via enteric neurons. The present study investigated the role of endogenous 5-HT and 5-HT3 receptors in the pathogenic mechanisms involved in colonic inflammation, especially in relation to substance P (SP) and the neuro...

journal_title：British journal of pharmacology

authors： Utsumi D,Matsumoto K,Amagase K,Horie S,Kato S

更新日期：2016-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:As a hallmark of glioblastoma multiforme (GBM), CD44 plays a crucial role in promoting glioblastoma stem cell (GSC) stemness phenotypes and multiple drug resistance. The therapeutic potential of CD44 has been validated by the clinical successes of several CD44 inhibitors, including antibodies and...

journal_title：British journal of pharmacology

authors： Wang C,Wang Z,Chen C,Fu X,Wang J,Fei X,Yan X,Xu R

更新日期：2020-07-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common age related neurodegenerative disease. Currently, there are no disease modifying drugs, existing therapies only offer short-term symptomatic relief. Two of the pathognomonic indicators of AD are the presence of extracellular protein aggregates consisting primarily of the Aβ ...

journal_title：British journal of pharmacology

authors： Kenche VB,Barnham KJ

更新日期：2011-05-01 00:00:00

abstract：:1. ZENECA ZD7288 (4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino) pyrimidinium chloride, formerly ICI D7288) is a novel sino-atrial node function modulator which selectively slows sinus node rate. Its effects on haemodynamic function have been studied in pentobarbitone anaesthetized dogs, in comparison with zat...

journal_title：British journal of pharmacology

authors： Rouse W,Johnson IR

更新日期：1994-11-01 00:00:00

abstract：:The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand propert...

journal_title：British journal of pharmacology

authors： Alexander SP,Peters JA,Kelly E,Marrion N,Benson HE,Faccenda E,Pawson AJ,Sharman JL,Southan C,Davies JA,CGTP Collaborators.

更新日期：2015-12-01 00:00:00

abstract：:1. In the present study, we describe the expression of the neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide (PACAP) as well as their receptors in PC-3 cells, a human prostate cancer cell line. In addition, we have investigated their role in apoptosis induced by s...

journal_title：British journal of pharmacology

authors： Gutiérrez-Cañas I,Rodríguez-Henche N,Bolaños O,Carmena MJ,Prieto JC,Juarranz MG

更新日期：2003-07-01 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：BACKGROUND AND PURPOSE:Humanized mice for the nuclear receptor peroxisome proliferator-activated receptor δ (PPARδ), termed PPARδ knock-in (PPARδ KI) mice, were generated for the investigation of functional differences between mouse and human PPARδ and as tools for early drug efficacy assessment. EXPERIMENTAL APPROACH...

journal_title：British journal of pharmacology

authors： Gross B,Hennuyer N,Bouchaert E,Rommens C,Grillot D,Mezdour H,Staels B

更新日期：2011-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibition of PDE5 improves synaptic plasticity and memory via enhancing cGMP expression, thus activating the cGMP/cAMP response element binding protein (CREB) signalling pathway. This study investigated the effects of a PDE5 inhibitor on scopolamine-induced cognitive dysfunction, using memory-re...

journal_title：British journal of pharmacology

authors： Zhang L,Seo JH,Li H,Nam G,Yang HO

更新日期：2018-08-01 00:00:00

abstract：:1 Post-tetanic potentiation (p.t.p.) of the compound action potential in the presence of hexamethonium was observed in the isolated stellate ganglion of the hamster using extracellular postganglionic recordings. 2 The magnitude of the p.t.p. was small (less than a 20% increase) in the control solution, but increased a...

journal_title：British journal of pharmacology

authors： Christ D

更新日期：1980-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GPR18 is a recently deorphaned lipid receptor that is activated by the endogenous lipid N-arachidonoyl glycine (NAGly) as well the behaviourally inactive atypical cannabinoid, abnormal cannabidiol (Abn-CBD). The presence and/or function of any GPR18-based ocular signalling system remain essential...

journal_title：British journal of pharmacology

authors： Caldwell MD,Hu SS,Viswanathan S,Bradshaw H,Kelly ME,Straiker A

更新日期：2013-06-01 00:00:00