Inhibition of TRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid.

abstract：BACKGROUND AND PURPOSE:2-Hydroxypropyl-β-cyclodextrin (HPCD) is an FDA approved vehicle for drug delivery and an efficient cholesterol-lowering agent. HPCD was proposed to lower tissue cholesterol via multiple mechanisms including those mediated by oxysterols. CYP27A1 and CYP46A1 are the major oxysterol-producing enzym...

journal_title：British journal of pharmacology

authors： El-Darzi N,Mast N,Petrov AM,Pikuleva IA

更新日期：2020-07-22 00:00:00

abstract：BACKGROUND AND PURPOSE:Nitric oxide (NO) is known to activate NO-sensitive guanylyl cyclase (NO-GC) and to elicit cGMP production. However, NO has also been proposed to induce cGMP-independent effects. It is accepted practice to use specific NO-GC inhibitors, such as ODQ or NS2028, to assess cGMP-dependent NO effects. ...

journal_title：British journal of pharmacology

authors： Lies B,Groneberg D,Gambaryan S,Friebe A

更新日期：2013-09-01 00:00:00

abstract：:1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-...

journal_title：British journal of pharmacology

authors： Snowdy S,Liang HX,Blackburn B,Lum R,Nelson M,Wang L,Pfister J,Sharma BP,Wolff A,Belardinelli L

更新日期：1999-01-01 00:00:00

abstract：:1. In rats under ether anaesthesia, the left coronary artery was ligated and reperfused after 10 min of ischaemia. Forty-eight hours later the myocardium was analyzed for creatine kinase (CK) activity. 2. Human superoxide dismutase (h-SOD) given 1 min after occlusion and again 6 h later significantly improved survival...

journal_title：British journal of pharmacology

authors： Aoki N,Bitterman H,Brezinski ME,Lefer AM

更新日期：1988-11-01 00:00:00

abstract：:1. The variation with clock-hour in the behaviour of naive rats in a Y-maze has been recorded.2. The number of entries recorded was highest during the light period while the number of faecal boluses was highest during the dark period. Rearing showed a biphasic periodicity.3. The responses to LSD, mescaline and ampheta...

journal_title：British journal of pharmacology

authors： Davies JA,Redfern PH

更新日期：1973-09-01 00:00:00

abstract：:1. A single i.p. injection of bacterial endotoxin in rats (3.5 mg kg-1) caused lung injury assessed as changes in lung dry:wet weight ratio and leukopaenia over the subsequent 28 h. 2. This treatment also slowed the efflux of 14C from [14C]-prostaglandin E2 (PGE2), i.e., increased t1/2 and increased the survival of PG...

journal_title：British journal of pharmacology

authors： Izumi T,Bakhle YS

更新日期：1988-04-01 00:00:00

abstract：:1. The effects of diprafenone and propafenone on transmembrane action potential were examined and compared in papillary muscles and single ventricular myocytes isolated from guinea-pig hearts. 2. In papillary muscles, both diprafenone and propafenone > or = 10(-6) M caused a significant and dose-dependent decrease in ...

journal_title：British journal of pharmacology

authors： Kodama I,Suzuki R,Honjo H,Toyama J

更新日期：1992-11-01 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：:Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment. In this study, the effects of TAK-147 at 2 mg kg(-1) p.o. for 21 days, compared t...

journal_title：British journal of pharmacology

authors： Hatip-Al-Khatib I,Iwasaki K,Yoshimitsu Y,Arai T,Egashira N,Mishima K,Ikeda T,Fujiwara M

更新日期：2005-08-01 00:00:00

abstract：:1. The subtype of alpha1-adrenoceptor mediating contractions to phenylephrine of the rat thoracic aorta, mesenteric artery and pulmonary artery were investigated by use of antagonists which show selectivity between the cloned alpha1-adrenoceptor subtypes in binding studies. 2. Cumulative concentration-contraction curv...

journal_title：British journal of pharmacology

authors： Hussain MB,Marshall I

更新日期：1997-11-01 00:00:00

abstract：:The smooth muscle relaxant responses to the mixed beta(3)-, putative beta(4)-adrenoceptor agonist, (-)-CGP 12177 in rat colon are partially resistant to blockade by the beta(3)-adrenoceptor antagonist SR59230A suggesting involvement of beta(3)- and putative beta(4)-adrenoceptors. We now investigated the function of th...

journal_title：British journal of pharmacology

authors： Oostendorp J,Preitner F,Moffatt J,Jimenez M,Giacobino JP,Molenaar P,Kaumann AJ

更新日期：2000-06-01 00:00:00

abstract：:1 Inactivation of prostaglandin E2 in the pulmonary circulation of rabbits in vivo was measured by comparing the hypotensive effects of doses given intravenously and intra-arterially. 2 Di-4-phloretin phosphate (DPP) 25-100 mug kg-1 min-1 inhibited the inactivation of prostaglandin E2 in the pulmonary circulation. 3 T...

journal_title：British journal of pharmacology

authors： Crutchley DJ,Piper PJ

更新日期：1975-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The aim of this study was to determine whether the apelin/APJ system is altered in human cardiovascular disease by investigating whether the expression of apelin or its receptor is altered at the protein level. EXPERIMENTAL APPROACH:Radioligand binding studies were used to determine apelin recep...

journal_title：British journal of pharmacology

authors： Pitkin SL,Maguire JJ,Kuc RE,Davenport AP

更新日期：2010-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Methylene blue (MB) is commonly employed as a treatment for methaemoglobinaemia, malaria and vasoplegic shock. An increasing number of studies indicate that MB can cause 5-HT toxicity when administered with a 5-HT reuptake inhibitor. MB is a potent inhibitor of monoamine oxidases, but other targe...

journal_title：British journal of pharmacology

authors： Oz M,Isaev D,Lorke DE,Hasan M,Petroianu G,Shippenberg TS

更新日期：2012-05-01 00:00:00

abstract：:1 The effects of alpha- and beta-adrenoceptor stimulants on the histamine-forming capacity (HFC) of human isolated leucocytes have been studied, in vitro.2 It was confirmed that antigen significantly stimulates the HFC of human leucocytes.3 beta-Adrenoceptor stimulants, such as isoprenaline and salbutamol (10(-6)-10(-...

journal_title：British journal of pharmacology

authors： Assem ES

更新日期：1974-10-01 00:00:00

abstract：:1. In this study, we compared two series of newly discovered ligands for their selectivity to benzodiazepine sites in the alpha 1 beta 2 gamma 2 and the alpha 6 beta 2 gamma 2 subtypes of cloned gamma-aminobutyric acidA (GABAA) receptors, the latter being unique in not interacting with classical benzodiazepines. 2. Th...

journal_title：British journal of pharmacology

authors： Im WB,Im HK,Pregenzer JF,Hamilton BJ,Carter DB,Jacobsen EJ,TenBrink RE,VonVoigtlander PF

更新日期：1993-10-01 00:00:00

abstract：:1. The effect on systemic haemodynamics of BQ-123, a selective endothelin A (ETA) receptor antagonist, was investigated in healthy men by giving, on separate occasions, ascending intravenous doses of 100, 300, 1000 and 3000 nmol min(-1) BQ-123, each for 15 min, in a randomized, placebo-controlled, double-blind study. ...

journal_title：British journal of pharmacology

authors： Spratt JC,Goddard J,Patel N,Strachan FE,Rankin AJ,Webb DJ

更新日期：2001-10-01 00:00:00

abstract：:1. The effect of the nitro-derivative of aspirin, NCX4016, was assessed on ischaemic ventricular arrhythmias and myocardial infarct size in anaesthetized pigs in comparison to native aspirin. 2. Pigs were given aspirin (10 mg kg(-1); n=6), low dose NCX4016 (18.4 mg kg(-1); n=6) or high dose NCX4016 (60 mg kg(-1); n=7)...

journal_title：British journal of pharmacology

authors： Wainwright CL,Miller AM,Work LM,Del Soldato P

更新日期：2002-04-01 00:00:00

abstract：:1 Ca(2+)-activated Cl(-) currents (I(Cl(Ca))) evoked by K(+)-free pipette solutions containing 500 nM Ca(2+) were recorded in rabbit pulmonary artery smooth muscle cells. A voltage step protocol in which the cells were stepped to +70 mV and then to -80 mV produced outward and inward Cl(-) currents respectively that ex...

journal_title：British journal of pharmacology

authors： Piper AS,Greenwood IA

更新日期：2003-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We investigated whether or not kinin receptors play a role in diabetic blood-retinal barrier breakdown, which is a leading cause of vision loss. EXPERIMENTAL APPROACH:Blood-retinal barrier breakdown was quantified using Evans blue, and expression of kinin B(1) receptor mRNA was measured using qu...

journal_title：British journal of pharmacology

authors： Abdouh M,Talbot S,Couture R,Hasséssian HM

更新日期：2008-05-01 00:00:00

abstract：:1 Histamine produced dose-dependent contractile responses on both isolated perfused ear arteries and aortic strips of the rabbit. These responses were blocked by mepyramine and potentiated by both metiamide and dithiothreitol. 2 In the presence of maximum potentiation by metiamide, dithiothreitol still potentiated the...

journal_title：British journal of pharmacology

authors： Carroll PR,Glover WE

更新日期：1977-02-01 00:00:00

abstract：:1. The vasodilator effects of arginine, nitric oxide (NO), acetylcholine (ACh) and sodium nitroprusside (NP) in the noradrenaline-preconstricted ('high tone') perfused rat kidney have been examined. 2. L-Arginine (0.6-23 mumol) caused a biphasic change in renal perfusion pressure. D-Arginine (0.6-23 mumol) was without...

journal_title：British journal of pharmacology

authors： Bhardwaj R,Moore PK

更新日期：1989-07-01 00:00:00

abstract：:Rodent models of chronic pain may elucidate pathophysiological mechanisms and identify potential drug targets, but whether they predict clinical efficacy of novel compounds is controversial. Several potential analgesics have failed in clinical trials, in spite of strong animal modelling support for efficacy, but there...

journal_title：British journal of pharmacology

authors： Berge OG

更新日期：2011-10-01 00:00:00

abstract：:1. To elucidate whether K+ channels play a role in the action of epithelium-dependent bronchodilatation, we studied responses in human bronchial strips in the presence of indomethacin and NG-nitro-L-arginine methylester under isometric conditions, in vitro. 2. Mechanical removal of the epithelium increased the contrac...

journal_title：British journal of pharmacology

authors： Tamaoki J,Tagaya E,Isono K,Kondo M,Konno K

更新日期：1997-06-01 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：BACKGROUND AND PURPOSE:Endocannabinoids play an important role in modulating spinal nociceptive signalling, crucial for the development of pain. The cannabinoid CB1 receptor and the TRPV1 cation channel are both activated by the endocannabinoid anandamide, a product of biosynthesis from the endogenous lipid precursor N...

journal_title：British journal of pharmacology

authors： Nerandzic V,Mrozkova P,Adamek P,Spicarova D,Nagy I,Palecek J

更新日期：2018-06-01 00:00:00

abstract：:G protein-coupled receptors are the largest group of membrane proteins and are the targets for approximately 30% of drugs currently used therapeutically. These 7-transmembrane-spanning proteins continue to provide new opportunities to develop therapeutics based on emerging knowledge of their structure, signalling prop...

journal_title：British journal of pharmacology

authors： Summers RJ

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Melanin-concentrating hormone receptor 1 (MCH1 receptor) antagonists are being considered as anti-obesity agents. The present study reports a new class of MCH1 receptor antagonists with an 8-methylquinoline scaffold. The molecular mechanism of MCH1 receptor blockade by these antagonists was exami...

journal_title：British journal of pharmacology

authors： Sakurai T,Ogawa K,Ishihara Y,Kasai S,Nakayama M

更新日期：2014-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hypoxia/reoxygenation induces synthesis of reactive oxygen species (ROS) which can attack macromolecules and cause brain injury. The transcription factor, nuclear factor (erythroid-derived 2)-like 2, (Nrf2), ia potent activator of genes with an antioxidant responsive element and Nrf2 can countera...

journal_title：British journal of pharmacology

authors： Cao S,Chao D,Zhou H,Balboni G,Xia Y

更新日期：2015-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled corticosteroids (ICS) are the cornerstone of asthma pharmacotherapy and, acting via the glucocorticoid receptor (GR), reduce inflammatory gene expression. While this is often attributed to a direct inhibitory effect of the GR on inflammatory gene transcription, corticosteroids also induce...

journal_title：British journal of pharmacology

authors： Kelly MM,King EM,Rider CF,Gwozd C,Holden NS,Eddleston J,Zuraw B,Leigh R,O'Byrne PM,Newton R

更新日期：2012-03-01 00:00:00