Quantification of the characteristics of antagonists exhibiting both competitive antagonism and functional interaction.

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：:Adrenergic transmission was investigated in the dog mesenteric vein by recording electrical responses of single smooth muscle cells to perivascular nerve stimulation. Perivascular nerve stimulation generated an excitatory junction potential (e.j.p.) and a slow depolarization of the membrane. The amplitude of the e.j.p...

journal_title：British journal of pharmacology

authors： Suzuki H

更新日期：1984-03-01 00:00:00

abstract：:1. Acetylcholine (ACh)-induced relaxation of aortic strips with endothelium and production of cyclic GMP between streptozotocin-induced diabetic and age-matched control rats were compared. 2. The concentration-response curve for ACh-induced relaxation was shifted to the right in diabetic rats. IC50 values for ACh were...

journal_title：British journal of pharmacology

authors： Kamata K,Miyata N,Kasuya Y

更新日期：1989-06-01 00:00:00

abstract：:The binding characteristics of the relaxin receptor in rat atria, uterus and cortex were studied using a [33P]-labelled human gene 2 relaxin (B33) and quantitative receptor autoradiography. The binding kinetics of [33P]-human gene 2 relaxin (B33) were investigated in slide-mounted rat atrial sections. The binding achi...

journal_title：British journal of pharmacology

authors： Tan YY,Wade JD,Tregear GW,Summers RJ

更新日期：1999-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In patients with pulmonary hypertension (PH) associated with lung disease and/or hypoxia (Group III), decreased pulmonary vascular tone and tissue hypoxia is therapeutically beneficial. PGE2 and PGI2 induce potent relaxation of human bronchi from non-PH (control) patients via EP4 and IP receptors...

journal_title：British journal of pharmacology

authors： Ozen G,Benyahia C,Mani S,Boukais K,Silverstein AM,Bayles R,Nelsen AC,Castier Y,Danel C,Mal H,Clapp LH,Longrois D,Norel X

更新日期：2020-01-01 00:00:00

abstract：:Pulmonary fibrosis represents the end stage of a number of heterogeneous conditions and is, to a greater or lesser degree, the hallmark of the interstitial lung diseases. It is characterized by the excessive deposition of extracellular matrix proteins within the pulmonary interstitium leading to the obliteration of fu...

journal_title：British journal of pharmacology

authors： Datta A,Scotton CJ,Chambers RC

更新日期：2011-05-01 00:00:00

abstract：:The complement system plays a major role in threat recognition and in orchestrating responses to microbial intruders and accumulating debris. This immune surveillance is largely driven by lectins that sense carbohydrate signatures on foreign, diseased and healthy host cells and act as complement activators, regulators...

journal_title：British journal of pharmacology

authors： Hevey R,Pouw RB,Harris C,Ricklin D

更新日期：2020-11-03 00:00:00

abstract：:1. Capsaicin, the irritant principle of hot peppers, is a vanilloid agonist known to activate the transient receptor potential channel vanilloid subfamily member 1 (VR1), recently reported to be involved in neurodegeneration. The present study investigated the role of VR1 in a model of global cerebral ischemia in gerb...

journal_title：British journal of pharmacology

authors： Pegorini S,Braida D,Verzoni C,Guerini-Rocco C,Consalez GG,Croci L,Sala M

更新日期：2005-03-01 00:00:00

abstract：:YM471, (Z)-4'-[4,4-difluoro-5-[2-(4-dimethylaminopiperidino)-2-oxoethylidene]-2,3,4,5-tetrahydro-1H-1-benzoazepine-1-carbonyl]-2-phenylbenzanilide monohydrochloride, is a newly synthesized potent vasopressin (AVP) receptor antagonist. Its effects on binding to and signal transduction by cloned human AVP receptors (V(1...

journal_title：British journal of pharmacology

authors： Tsukada J,Tahara A,Tomura Y,Wada Ki,Kusayama T,Ishii N,Yatsu T,Uchida W,Taniguchi N,Tanaka A

更新日期：2001-07-01 00:00:00

abstract：:1. Vasospasm of arterial conduits used for coronary artery surgery is an important cause of graft failure and is likely to result partly from raised levels of vasoconstrictor substances such as thromboxane A(2) and endothelin-1. Our aim was to find pharmacological agents that could prevent agonist-induced vasospasm. 2...

journal_title：British journal of pharmacology

authors： Batchelor TJ,Sadaba JR,Ishola A,Pacaud P,Munsch CM,Beech DJ

更新日期：2001-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The anti-cancer agent [Arg(6), D-Trp(7,9), N(me)Phe(8)]-substance P (6-11) (SP-G) modulates gastrin releasing peptide (GRP) and arginine vasopressin signalling in small cell lung cancer cells leading to growth arrest and apoptosis. We have shown that SP-G acts as a biased agonist at GRP receptors...

journal_title：British journal of pharmacology

authors： MacKinnon AC,Tufail-Hanif U,Wheatley M,Rossi AG,Haslett C,Seckl M,Sethi T

更新日期：2009-01-01 00:00:00

abstract：:1. The contribution of nitric oxide (NO) and vasoactive intestinal polypeptide (VIP) to non-adrenergic non-cholinergic (NANC) relaxations in the pig gastric fundus was investigated. 2. Circular and longitudinal muscle strips were mounted for isotonic registration in the presence of atropine and guanethidine; tone was ...

journal_title：British journal of pharmacology

authors： Lefebvre RA,Smits GJ,Timmermans JP

更新日期：1995-10-01 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：BACKGROUND AND PURPOSE:Inhibitors of histone deacetylase (HDAC) are emerging as a promising class of anti-cancer drugs, but a generic deregulation of transcription in neoplastic cells cannot fully explain their therapeutic effects. In this study we evaluated alternative molecular mechanisms by which HDAC inhibitors cou...

journal_title：British journal of pharmacology

authors： Condorelli F,Gnemmi I,Vallario A,Genazzani AA,Canonico PL

更新日期：2008-02-01 00:00:00

abstract：:The release of gamma-aminobutyric acid (GABA) and acetylcholine (ACh) from the strips of guinea-pig ileum was investigated in the presence of neurotensin. Neurotensin evoked the release of [3H]-GABA from the strips preloaded with [3H]-GABA, and the evoked release was Ca2+-dependent and tetrodotoxin-sensitive. Hexameth...

journal_title：British journal of pharmacology

authors： Nakamoto M,Tanaka C,Taniyama K

更新日期：1987-03-01 00:00:00

abstract：:The effects of the opioid receptor agonist RX783006 and of the opioid receptor partial agonist (+)-meptazinol have been examined on electrically induced twitch responses of the guinea-pig isolated ileum and of the mouse isolated vas deferens. Log10 concentration-tissue state curves were determined for (+)-meptazinol a...

journal_title：British journal of pharmacology

authors： Goodall J,Hughes IE,Mackay D

更新日期：1986-07-01 00:00:00

abstract：:1. Aggressive behaviour was elicited in rats that had been deprived of food for 20 h daily (starved), by chronic administration of Cannabis sativa extract or (-)-Delta(9)-trans-tetrahydrocannabinol.2. The influence of intraperitoneal (i.p.) or oral glucose administration, cold environment, acidosis, and corn, and prot...

journal_title：British journal of pharmacology

authors： Carlini EA,Hamaoui A,Märtz RM

更新日期：1972-04-01 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：:1. Chronic inhibition of nitric oxide synthase (NOS) provokes a hypertensive state which has been shown to be angiotensin II (Ang-II) dependent. In addition to raising blood pressure, NOS inhibition also causes leukocyte adhesion. The present study was designed to define the role of Ang-II in hypertension and in the l...

journal_title：British journal of pharmacology

authors： Alvarez A,Piqueras L,Bello R,Canet A,Moreno L,Kubes P,Sanz MJ

更新日期：2001-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Small conductance calcium-activated potassium (KCa 2.x) channels have a widely accepted canonical function in regulating cellular excitability. In this study, we address a potential non-canonical function of KCa 2.x channels in breast cancer cell survival, using in vitro models. EXPERIMENTAL APP...

journal_title：British journal of pharmacology

authors： Abdulkareem ZA,Gee JM,Cox CD,Wann KT

更新日期：2016-01-01 00:00:00

abstract：:1. We studied the effect of bradykinin on plasma exudation in the airways of the anaesthetized guinea-pig in vivo. Tissue content of extravasated Evans blue dye was used as an index of protein exudation in the larynx, trachea, main bronchi and intrapulmonary airways (i.p.a.). 2. Bradykinin increased the content of Eva...

journal_title：British journal of pharmacology

authors： Rogers DF,Dijk S,Barnes PJ

更新日期：1990-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Hydrogen sulphide (H(2) S) is gaining acceptance as a gaseous signal molecule. However, mechanisms regarding signal termination are not understood. We used stigmatellin and antimycin A, inhibitors of sulphide quinone reductase (SQR), to test the hypothesis that the catabolism of H(2) S involves S...

journal_title：British journal of pharmacology

authors： Linden DR,Furne J,Stoltz GJ,Abdel-Rehim MS,Levitt MD,Szurszewski JH

更新日期：2012-04-01 00:00:00

abstract：:The study was undertaken to investigate the 5-HT receptor mediating the inhibitory effect of 5-HT on peristalsis in the guinea-pig isolated ileum. The facilitatory and inhibitory effects were measured as the decrease and increase, respectively, in the intraluminal pressure required to trigger peristalsis. In the prese...

journal_title：British journal of pharmacology

authors： Tuladhar BR,Ge L,Naylor RJ

更新日期：2003-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT receptor agonists have variable nociceptive effects within the spinal cord. While there is some evidence for 5-HT(1A) spinally-mediated analgesia, the role of other 5-HT(1) receptor subtypes remains unclear. In the present study, we examined the spinal actions of a range of 5-HT(1) agonists,...

journal_title：British journal of pharmacology

authors： Jeong HJ,Mitchell VA,Vaughan CW

更新日期：2012-03-01 00:00:00

abstract：:1. ATP, UTP, ADP and ADP-beta-S elicited Ca2+ -signals in cultured aortic smooth muscle cells although ADP, UDP and ADP-beta-S gave approximately 40% of the maximal response seen with ATP and UTP. Adenosine, AMP or alpha,beta-methylene-ATP had no effect. These responses were attributed to P2Y2/4 and P2Y1 receptors, wh...

journal_title：British journal of pharmacology

authors： Pediani JD,McGrath JC,Wilson SM

更新日期：1999-04-01 00:00:00

abstract：:The discovery of the nitric oxide/cGMP pathway was the basis for our understanding of many normal physiological functions and the pathophysiology of several diseases. Since the discovery and introduction of sildenafil, inhibitors of PDE5 have been the first-line therapy for erectile dysfunction (ED). The success of si...

journal_title：British journal of pharmacology

authors： Andersson KE

更新日期：2018-07-01 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：:G protein-coupled receptors are one of the most actively studied families of proteins. However, despite the ubiquity of protein dimerization and oligomerization as a structural and functional motif in biology, until the last decade they were generally considered as monomeric, non-interacting polypeptides. For the meta...

journal_title：British journal of pharmacology

authors： Milligan G

更新日期：2008-03-01 00:00:00

abstract：:Dopamine, noradrenaline (NA) and adrenaline (Ad) depletion by 6-hydroxydopamine (6-OHDA) and pargyline plus 6-OHDA was investigated in the cat left ventricle, mesenteric and renal arteries, renal cortex, renal medulla and adrenal medulla. Catecholamine concentrations in plasma were also analyzed in these two experimen...

journal_title：British journal of pharmacology

authors： Caramona MM,Soares-da-Silva P

更新日期：1985-10-01 00:00:00

abstract：:1 The effect of methylene, thio, and imido substituted analogues of adenosine 5'-triphosphate (ATP) on surfactant phospholipid secretion and calcium mobilization in rat isolated alveolar Type II cells was studied. 2 ATP was the most potent secretagogue of adenine nucleotides studied. The rank order of agonist potency ...

journal_title：British journal of pharmacology

authors： Rice WR,Singleton FM

更新日期：1987-08-01 00:00:00