Characterization of adenosine receptors in guinea-pig isolated left atria.

abstract：:Perivascular adipose tissue (PVAT) is now recognized as an active player in vascular homeostasis. The expansion of PVAT in obesity and its possible role in vascular dysfunction have attracted much interest. In terms of the regulation of vascular tone and blood pressure, PVAT has been shown to release vasoactive mediat...

journal_title：British journal of pharmacology

authors： Ramirez JG,O'Malley EJ,Ho WSV

更新日期：2017-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The regulation of vascular soluble guanylyl cyclase (sGC) expression by nitric oxide (NO) is still under discussion. In vitro, NO has been shown to downregulate the expression of sGC but it is unclear if this mechanism is operative in vivo and occurs during nitrate treatment. EXPERIMENTAL APPROA...

journal_title：British journal of pharmacology

authors： Oppermann M,Dao VT,Suvorava T,Bas M,Kojda G

更新日期：2008-10-01 00:00:00

abstract：:The effects of the angiotensin-converting-enzyme inhibitor (ACEI) ramiprilat, the angiotensin II type 1 receptor antagonist (AT(1)A) candesartan, and the combination of both drugs on infarct size (IS) resulting from regional myocardial ischaemia were studied in pigs. Both ACEI and AT(1)A reduce myocardial IS by a brad...

journal_title：British journal of pharmacology

authors： Weidenbach R,Schulz R,Gres P,Behrends M,Post H,Heusch G

更新日期：2000-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sphingosine 1-phosphate (S1P), an important inflammatory mediator, has been shown to regulate COX-2 production and promote various cellular responses such as cell migration. Mevastatin, an inhibitor of 3-hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA), effectively inhibits inflammatory responses...

journal_title：British journal of pharmacology

authors： Hsu CK,Lin CC,Hsiao LD,Yang CM

更新日期：2015-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:This study investigated the role of central sympathetic activity and related mitogen-activated protein kinase (MAPK) signalling in the cardiovascular effects of ethanol in a model of acute renal failure (ARF). EXPERIMENTAL APPROACH:The effects of pharmacological interventions that inhibit periph...

journal_title：British journal of pharmacology

authors： El-Mas MM,El-Gowelli HM,Ghazal AR,Harraz OF,Mohy El-Din MM

更新日期：2009-11-01 00:00:00

abstract：:1. We have investigated the inhibitory effects of RP 73401 (piclamilast) and rolipram against human monocyte cyclic AMP-specific phosphodiesterase (PDE4) in relation to their effects on prostaglandin (PG)E2-induced cyclic AMP accumulation and lipopolysaccharide (LPS)-induced TNF alpha production and TNF alpha mRNA exp...

journal_title：British journal of pharmacology

authors： Souness JE,Griffin M,Maslen C,Ebsworth K,Scott LC,Pollock K,Palfreyman MN,Karlsson JA

更新日期：1996-06-01 00:00:00

abstract：UNLABELLED:Sensory neurons play important roles in many disorders, including inflammatory diseases, such as sepsis. Sepsis is a potentially lethal systemic inflammatory reaction to a local bacterial infection, affecting thousands of patients annually. Although associated with a high mortality rate, sepsis outcome depen...

journal_title：British journal of pharmacology

authors： Bodkin JV,Fernandes ES

更新日期：2013-12-01 00:00:00

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：:1. RS-15385-197 ((8aR, 12aS, 13aS)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulphonyl)-6H-isoquino [2,1-g][1,6]-naphthyridine) was evaluated in a series of in vitro and in vivo tests as an antagonist at alpha 2-adrenoceptors. 2. RS-15385-197 had a pKi of 9.45 for alpha 2-adrenoceptors in the rat cor...

journal_title：British journal of pharmacology

authors： Brown CM,MacKinnon AC,Redfern WS,Hicks PE,Kilpatrick AT,Small C,Ramcharan M,Clague RU,Clark RD,MacFarlane CB

更新日期：1993-02-01 00:00:00

abstract：:Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonar...

journal_title：British journal of pharmacology

authors： Marsango S,Barki N,Jenkins L,Tobin AB,Milligan G

更新日期：2020-09-01 00:00:00

abstract：:1. It has been suggested that the vasoconstrictor response to neuropeptide Y (NPY) is located in the microvessels and that it increases with reduced vessel diameter. The aim of the present study was to analyse quantitatively, on the cat gastrocnemius muscle preparation in vivo, the effects of NPY on total regional vas...

journal_title：British journal of pharmacology

authors： Ekelund U,Erlinge D

更新日期：1997-02-01 00:00:00

abstract：:1. Experiments were performed with peptidase inhibitors on rabbit aortic strip preparations, to determine whether endogenous peptidase activity can influence the potency estimates for angiotensin receptor agonists and antagonists in this tissue. 2. Angiotensin II (A II) and angiotensin III (A III) both induced concent...

journal_title：British journal of pharmacology

authors： Robertson MJ,Cunoosamy MP,Clark KL

更新日期：1992-05-01 00:00:00

abstract：:The effects of treatment with rolipram, a specific phosphodiesterase IV inhibitor, on learning and memory function and on the cyclic AMP/PKA/CREB signal transduction system were examined in rats with microsphere embolism (ME)-induced cerebral ischaemia. Sustained cerebral ischaemia was induced by the injection of 900 ...

journal_title：British journal of pharmacology

authors： Nagakura A,Niimura M,Takeo S

更新日期：2002-04-01 00:00:00

abstract：:Mouse spiders represent a potential cause of serious envenomation in humans. This study examined the activity of Missulena bradleyi venom in several in vitro preparations. Whilst female M. bradleyi venom at doses up to 0.05 microl ml(-1) failed to alter twitch or resting tension in all preparations used, male venom (0...

journal_title：British journal of pharmacology

authors： Rash LD,Birinyi-Strachan LC,Nicholson GM,Hodgson WC

更新日期：2000-08-01 00:00:00

abstract：:1. To clarify the role of the first thrombin receptor/protease-activated receptor (PAR)-1 in an inflammatory process, we tested and characterized the effect of intraplantar (i.pl.) administration of the highly specific PAR-1 agonist TFLLR-NH2 in rat hindpaw. 2. TFLLR-NH2 administered i.pl. at 0.01-0.03 micromol per pa...

journal_title：British journal of pharmacology

authors： Kawabata A,Kuroda R,Nishikawa H,Asai T,Kataoka K,Taneda M

更新日期：1999-04-01 00:00:00

abstract：:1 Pinacidil relaxes blood vessels through opening the K(ATP) channels with a resultant membrane hyperpolarization and inhibition of Ca(2+) influx. The aim of this study was to examine the mechanisms thereby pinacidil induces K(+) channel-independent relaxation in isolated endothelium-denuded rat mesenteric artery. 2 P...

journal_title：British journal of pharmacology

authors： Tsang SY,Yao X,Wong CM,Au CL,Chen ZY,Huang Y

更新日期：2003-02-01 00:00:00

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：:1 U46619, a prostaglandin H2 endoperoxide analogue and thromboxane A2 agonist, dose-dependently inhibited accumulation and metabolism of thromboxane B2 in the isolated perfused lung of the guinea-pig. At similar doses prostaglandins E1, E2, F1 alpha, F2 alpha, I2, 5, 6-trans-PGE2 and 8-iso-PGE1 were ineffective. 2 U46...

journal_title：British journal of pharmacology

authors： Hoult JR,Robinson C

更新日期：1983-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GoSlo-SR compounds are efficacious BK (KCa 1.1) channel openers, but little is known about their mechanism of action or effect on bladder contractility. We examined the effects of two closely related compounds on BK currents and bladder contractions. EXPERIMENTAL APPROACH:A combination of electr...

journal_title：British journal of pharmacology

authors： Large RJ,Kshatri A,Webb TI,Roy S,Akande A,Bradley E,Sergeant GP,Thornbury KD,McHale NG,Hollywood MA

更新日期：2015-05-01 00:00:00

abstract：:The aim of this study was to evaluate the potency of YM-53601 ((E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a new inhibitor of squalene synthase, in reducing both plasma cholesterol and triglyceride levels, compared with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase in...

journal_title：British journal of pharmacology

authors： Ugawa T,Kakuta H,Moritani H,Matsuda K,Ishihara T,Yamaguchi M,Naganuma S,Iizumi Y,Shikama H

更新日期：2000-09-01 00:00:00

abstract：:1. The effector mechanism of intestinal necrosis in rat anaphylaxis was studied following several complementary approaches: (i) the use of monoclonal antibodies (mAb) belonging to different classes (IgG1, IgG2b and IgE anti-DNP), (ii) the assay of mediators, and (iii) the use of pharmacological tools. 2. Lethality and...

journal_title：British journal of pharmacology

authors： Pellón MI,Steil AA,Furió V,Sánchez Crespo M

更新日期：1994-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:AZ11645373 and N-{2-methyl-5-[(1R, 5S)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-ylcarbonyl]phenyl}-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide hydrochloride (compound-22) are recently described P2X(7) receptor antagonists. In this study we have further characterized these compounds to determine their mecha...

journal_title：British journal of pharmacology

authors： Michel AD,Ng SW,Roman S,Clay WC,Dean DK,Walter DS

更新日期：2009-04-01 00:00:00

abstract：:The kallikrein-kinin system is subdivided into the plasma and tissue-kallikrein-kinin system, with bradykinin (BK) and kallidin (KAL) (Lys(0)-bradykinin) as functional peptides. This occurs in both humans and other mammals. Both peptides are released by plasma and tissue-kallikrein. BK, but not KAL, has been detected ...

journal_title：British journal of pharmacology

authors： Hilgenfeldt U,Stannek C,Lukasova M,Schnölzer M,Lewicka S

更新日期：2005-12-01 00:00:00

abstract：:It has been proposed that the vagus nerve plays a role in mediating cholecystokinin-8 (CCK-8) effect on such gastric functions as motility, emptying and gastric acid secretion. To examine the contribution of the efferent pathways in realizing these effects, efferent mass activity in the ventral gastric vagal nerve in ...

journal_title：British journal of pharmacology

authors： Bucinskaite V,Kurosawa M,Lundeberg T

更新日期：2000-04-01 00:00:00

abstract：:Binding of the 5-HT(7) receptor antagonist radioligand [(3)H]-SB-269970 to human 5-HT(7(a)) receptors expressed in HEK293 cell membranes (h5-HT(7(a))/293) and to guinea-pig cerebral cortex membranes, was characterized and compared with [(3)H]-5-CT binding. [(3)H]-SB-269970 (1 nM) showed full association with h5-HT(7(a...

journal_title：British journal of pharmacology

authors： Thomas DR,Atkinson PJ,Ho M,Bromidge SM,Lovell PJ,Villani AJ,Hagan JJ,Middlemiss DN,Price GW

更新日期：2000-05-01 00:00:00

abstract：:Antihistamine induced cognitive decline was evaluated using positron emission tomography (PET) measurement of histamine H1 receptor (H1R) occupancy and regional cerebral blood flow (rCBF). Cognitive performance in attention-demanding task deteriorated dose-dependently and the effects were statistically significant aft...

journal_title：British journal of pharmacology

authors： Okamura N,Yanai K,Higuchi M,Sakai J,Iwata R,Ido T,Sasaki H,Watanabe T,Itoh M

更新日期：2000-01-01 00:00:00

abstract：:1. The effects of intradermally injected prostaglandins (PGs) E(1), E(2), F(1alpha) and F(2alpha) have been examined in the rat and in man.2. PGE(1) and PGE(2) caused an increase in local vascular permeability in rat skin; their potency was comparable with that of other putative mediators of inflammation (histamine, b...

journal_title：British journal of pharmacology

authors： Crunkhorn P,Willis AL

更新日期：1971-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The endocannabinoid, anandamide, has anti-arrhythmic effects. The aim of the present study was to explore the electrophysiological effects of anandamide on rat myocardium. EXPERIMENTAL APPROACH:Evoked action potentials (APs) were recorded using intracellular recording technique in rat cardiac pa...

journal_title：British journal of pharmacology

authors： Li Q,Ma HJ,Zhang H,Qi Z,Guan Y,Zhang Y

更新日期：2009-12-01 00:00:00

abstract：:1 In the isolated kidney of the rabbit perfused with oxygenated Tyrode solution, we studied the effect of bradykinin on the vasoconstriction evoked by sympathetic nerve stimulation (3Hz, 1 ms) and by injections of noradrenaline (50 to 75 ng) in the presence and in the absence of indomethacin (1 microgram/ml), an inhib...

journal_title：British journal of pharmacology

authors： Malik KU,Nasjletti A

更新日期：1979-10-01 00:00:00

abstract：:1. Electroconvulsive treatment (ECT) of rabbits produced ocular inflammation consisting of conjunctival hyperaemia, miosis and protein extravasation into the aqueous humour, reflected by the so-called aqueous flare response (AFR): the maximal reduction in pupil size was 3.8 +/- 0.1 mm (s.e. of mean, n = 16) while the ...

journal_title：British journal of pharmacology

authors： Wang ZY,Waldeck K,Grundemar L,Håkanson R

更新日期：1997-04-01 00:00:00