Adrenomedullin 2/intermedin: a putative drug candidate for treatment of cardiometabolic diseases.

abstract：:1. Microfluorimetry techniques with fura-2 were used to characterize the effects of efaroxan (200 microM), phenotolamine (200-500 microM) and idazoxan (200-500 microM) on the intracellular free Ca2+ concentration ([Ca2+]i) in mouse isolated islets of Langerhans. 2. The imidazoline receptor agonists efaroxan and phento...

journal_title：British journal of pharmacology

authors： Shepherd RM,Hashmi MN,Kane C,Squires PE,Dunne MJ

更新日期：1996-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sphingosine-1-phosphate (S1P) has been shown to be involved in the asthmatic disease as well in preclinical mouse experimental models of this disease. The aim of this study was to understand the mechanism(s) underlying S1P effects on the lung. EXPERIMENTAL APPROACH:BALB/c, mast cell-deficient an...

journal_title：British journal of pharmacology

authors： Roviezzo F,Sorrentino R,Bertolino A,De Gruttola L,Terlizzi M,Pinto A,Napolitano M,Castello G,D'Agostino B,Ianaro A,Sorrentino R,Cirino G

更新日期：2015-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We recently reported that AAV1-Rheb(S16H) transduction could protect hippocampal neurons through the induction of brain-derived neurotrophic factor (BDNF) in the rat hippocampus in vivo. It is still unclear how neuronal BDNF produced by AAV1-Rheb(S16H) transduction induces neuroprotective effects...

journal_title：British journal of pharmacology

authors： Jeon MT,Moon GJ,Kim S,Choi M,Oh YS,Kim DW,Kim HJ,Lee KJ,Choe Y,Ha CM,Jang IS,Nakamura M,McLean C,Chung WS,Shin WH,Lee SG,Kim SR

更新日期：2020-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pelitinib is a potent irreversible EGFR TK inhibitor currently in clinical trials for the treatment of lung cancer. Hyperthermia has been applied concomitantly with chemotherapy and radiotherapy to enhance treatment outcome. In this study, we investigated the ability of the combination of pelitin...

journal_title：British journal of pharmacology

authors： To KK,Poon DC,Wei Y,Wang F,Lin G,Fu L

更新日期：2015-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Gain of function mutations in TRPC6 channels can cause autosomal dominant forms of focal segmental glomerulosclerosis (FSGS). Validated inhibitors of TRPC6 channels that are biologically active on FSGS-related TRPC6 mutants are eagerly sought. EXPERIMENTAL APPROACH:We synthesized new TRPC6-inhib...

journal_title：British journal of pharmacology

authors： Urban N,Neuser S,Hentschel A,Köhling S,Rademann J,Schaefer M

更新日期：2017-11-01 00:00:00

abstract：:1. The effect of basal tension (transmural tensions 235 +/- 29 mg wt (low tension: equivalent to approximately 16 mmHg) and 305 +/- 34 mg wt (high tension: equivalent to 35 mmHg)) on rat pulmonary resistance artery responses to endothelin-1 (ET-1) and the selective ET(B)-receptor agonist sarafotoxin S6c (S6c) were stu...

journal_title：British journal of pharmacology

authors： MacLean MR,McCulloch KM

更新日期：1998-03-01 00:00:00

abstract：:The past two decades have seen an immense increase in our appreciation of the vast range of signalling processes and supporting machinery that occur in cells. Pivotal to this is the notion of signal compartmentalization (compartmentation). Targeting by protein domains is critical in allowing signalling complexes to be...

journal_title：British journal of pharmacology

authors： Houslay MD

更新日期：2009-09-01 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：:Immersion of the hind paws of anesthetized rats in hot water for 5 min induced massive plasma protein leakage as indicated by extravasation of Evans blue dye in the skin. The threshold temperature which caused noticeable plasma extravasation was 45 degrees C, a maximal response was obtained between 55 degrees C and 60...

journal_title：British journal of pharmacology

authors： Saria A

更新日期：1984-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

journal_title：British journal of pharmacology

authors： Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

更新日期：2012-09-01 00:00:00

abstract：:Strips of human pulmonary arteries from patients undergoing surgery for lung tumour were incubated with [3H]-noradrenaline. Subsequently, they were superfused with physiological salt solution containing cocaine and corticosterone. Tritium overflow from the strips was stimulated by transmural electrical impulses (2 Hz)...

journal_title：British journal of pharmacology

authors： Göthert M,Hentrich F

更新日期：1985-08-01 00:00:00

abstract：:1. An antisense approach to block nitric oxide (NO) synthesis was developed, complementing the widely used chemical inhibitors and overcoming problems associated with their use in studying the roles of NO. 2. Murine macrophage cell lines (J774.2) were generated expressing a 500 bp sequence from inducible NO synthase (...

journal_title：British journal of pharmacology

authors： Cartwright JE,Johnstone AP,Whitley GS

更新日期：1997-01-01 00:00:00

abstract：:1. The aims of this study were first, to examine whether deficits in nerve conduction in streptozotocin-diabetic rats could be reversed by a 10% dietary supplement of evening primrose oil. Second, to determine the time-course of reversal, and third, to assess whether the effects could be blocked by the cyclo-oxygenase...

journal_title：British journal of pharmacology

authors： Cameron NE,Cotter MA,Dines KC,Robertson S,Cox D

更新日期：1993-08-01 00:00:00

abstract：:1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency...

journal_title：British journal of pharmacology

authors： Newbould BB

更新日期：1969-03-01 00:00:00

abstract：:1. The effects of alpha 2-adrenoceptor and kappa-opiate receptor activation on 45Ca accumulation into rat cortical synaptosomes were examined. 2. Clonidine (1 microM) and U50488H (1 microM) significantly reduced 45Ca accumulation under both resting (5 mM K+) and depolarizing (15-30 mM K+) conditions. 3. The inhibitory...

journal_title：British journal of pharmacology

authors： Xiang JZ,Brammer MJ,Campbell IC

更新日期：1990-09-01 00:00:00

abstract：:1. The concentrations of 5-hydroxytryptamine (5-HT), 5-hydroxyindolacetic acid (5-HIAA) and noradrenaline (NA) in homogenized rat brains were determined after intraperitoneal injection of 1,2,3,4-tetrahydro-2-naphthylamine (THN).2. THN caused a decrease in the concentration of brain 5-HIAA without altering its 5-HT co...

journal_title：British journal of pharmacology

authors： Bruinvels J

更新日期：1971-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Marijuana smoking is widespread in many countries, and the use of smoked synthetic cannabinoids is increasing. Smoking a marijuana joint leads to bronchodilation in both healthy subjects and asthmatics. The effects of Δ(9) -tetrahydrocannabinol and synthetic cannabinoids on human bronchus reactiv...

journal_title：British journal of pharmacology

authors： Grassin-Delyle S,Naline E,Buenestado A,Faisy C,Alvarez JC,Salvator H,Abrial C,Advenier C,Zemoura L,Devillier P

更新日期：2014-06-01 00:00:00

abstract：:1. We compared the relaxant effect of pituitary adenylate cyclase activating peptide (PACAP) 1-27 with that of a newly developed PACAP 1-27 analogue, [Arg15,20,21Leu17]-PACAP-Gly-Lys-Arg-NH2, in the guinea-pig trachea and primate bronchi in vitro (n = 4-5). 2. In the guinea-pig trachea precontracted by a submaximally ...

journal_title：British journal of pharmacology

authors： Yoshihara S,Lindén A,Kashimoto K,Nagano Y,Ichimura T,Nadel JA

更新日期：1997-08-01 00:00:00

abstract：:1. The present work describes the effects of inhibitors (amiloride and ethylisopropylamiloride) and activators (quinoxaline and phenylephrine) of the Na(+)-H+ exchanger on the outflow of dopamine in rat kidney slices loaded with L-dihydroxyphenylalanine (L-DOPA). 2. Incubation of kidney slices loaded with 50 microM L-...

journal_title：British journal of pharmacology

authors： Soares-da-Silva P

更新日期：1993-06-01 00:00:00

abstract：:1. The antithrombotic action of argatroban, a synthetic thrombin inhibitor, was studied in a canine model of coronary cyclic flow having some of the characteristics of acute unstable angina. Heparin was studied as a reference anticoagulant. 2. Localized endothelial damage was induced in the circumflex coronary artery ...

journal_title：British journal of pharmacology

authors： Duval N,Lunven C,O'Brien DP,Grosset A,O'Connor SE,Berry CN

更新日期：1996-06-01 00:00:00

abstract：:1. The kinetics of glycine-sensitive, N-methyl-D-aspartate (NMDA) receptor desensitization were investigated in cultured neurones with the patch clamp technique. 2. The degree of fast NMDA-receptor desensitization was inversely related to glycine concentration. Thus, increasing concentrations of glycine from 30 nM to ...

journal_title：British journal of pharmacology

authors： Parsons CG,Zong X,Lux HD

更新日期：1993-05-01 00:00:00

abstract：:1. The present study was aimed at elucidating the apoptosis inhibitory properties of the cyanoguanidine CHS 828. CHS 828 exhibits impressive cytotoxic activity in vitro and in vivo. Apoptosis is not its main mode of cytotoxic effect, and we have previously proposed a dual mechanism, where CHS 828 inhibits its own cell...

journal_title：British journal of pharmacology

authors： Martinsson P,Ekelund S,Nygren P,Larsson R

更新日期：2002-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Depolarization-induced suppression of inhibition (DSI) and excitation (DSE) are two forms of cannabinoid CB(1) receptor-mediated inhibition of synaptic transmission, whose durations are regulated by endocannabinoid (eCB) degradation. We have recently shown that in cultured hippocampal neurons mon...

journal_title：British journal of pharmacology

authors： Straiker A,Wager-Miller J,Hu SS,Blankman JL,Cravatt BF,Mackie K

更新日期：2011-11-01 00:00:00

abstract：:1. The role of nitric oxide in the coronary circulation under basal conditions and when exposed to various vasodilator stimuli was studied in instrumented, anaesthetized goats, by examining the action of inhibiting endogenous nitric oxide production with NG-nitro-L-arginine methyl ester (L-NAME). 2. In 12 goats, left ...

journal_title：British journal of pharmacology

authors： García JL,Fernández N,García-Villalón AL,Monge L,Gómez B,Diéguez G

更新日期：1992-07-01 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：BACKGROUND AND PURPOSE:The aim of the present study was to assess the interaction of nitrergic neurotransmission within the bed nucleus of the stria terminalis (BNST) with local glutamatergic and noradrenergic neurotransmission in the control of cardiovascular responses to acute restraint stress in rats. EXPERIMENTAL ...

journal_title：British journal of pharmacology

authors： Barretto-de-Souza L,Adami MB,Benini R,Crestani CC

更新日期：2018-10-01 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. Caffeine, 0.6-20.0 mM, altered the duration of the action potential recorded from kitten papillary muscles; low concentrations shortened and high concentrations prolonged the action potential.2. Caffeine, 20 mM, prolonged the action potential by delaying the final phase of repolarization.3. Caffeine, 2.0-20.0 mM in...

journal_title：British journal of pharmacology

authors： Clark A,Olson CB

更新日期：1973-01-01 00:00:00

abstract：:1 Contractile responses produced by the alpha 1-adrenoceptor selective agonist, phenylephrine, and the alpha 2-adrenoceptor selective agonists, oxymetazoline and clonidine, have been compared to those produced by noradrenaline (non selective) in the rat aorta. 2 The relative order of potency of the agonists was noradr...

journal_title：British journal of pharmacology

authors： Godfraind T,Miller RC,Lima JS

更新日期：1982-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Fibrosis, a pathological accumulation of collagen in tissues, represents a major global disease burden. Effective characterization of potential antifibrotic drugs has been constrained by poor formation of the extracellular matrix in vitro, due to tardy procollagen processing by collagen C-protein...

journal_title：British journal of pharmacology

authors： Chen CZ,Peng YX,Wang ZB,Fish PV,Kaar JL,Koepsel RR,Russell AJ,Lareu RR,Raghunath M

更新日期：2009-11-01 00:00:00