In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.

abstract：:1. FPL 67156 (6-N,N-diethyl-beta, gamma-dibromomethylene-D-ATP), is a newly synthesized analogue of ATP. 2. In a rabbit isolated tracheal epithelium preparation, measuring P2U-purinoceptor-dependent chloride secretion, FPL 67156 was discovered to potentiate the responses to UTP but not those to ATP-gamma-S. UTP agonis...

journal_title：British journal of pharmacology

authors： Crack BE,Pollard CE,Beukers MW,Roberts SM,Hunt SF,Ingall AH,McKechnie KC,IJzerman AP,Leff P

更新日期：1995-01-01 00:00:00

abstract：:1. Strength-duration curves for threshold mechanical responses to single transmural stimuli were identical for rat and guinea-pig detrusor. In both species atropine had no effect on the curves, but the curves were shifted to the right by nerve blockade with tetrodotoxin (TTX), and by blockade of P2-purinoceptors with ...

journal_title：British journal of pharmacology

authors： Brading AF,Williams JH

更新日期：1990-03-01 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：:Amyotrophic lateral sclerosis (ALS) is an adult-onset neurodegenerative disease characterized by the selective death of upper and lower motor neurons which ultimately leads to paralysis and ultimately death. Pathological changes in ALS are closely associated with pronounced and progressive changes in mitochondrial mor...

journal_title：British journal of pharmacology

authors： Muyderman H,Chen T

更新日期：2014-04-01 00:00:00

abstract：:1. gamma-Aminobutyric acid (GABA) was applied by the 'concentration clamp' technique to isolated neurones of Aplysia. GABA induced a chloride current (ICl) due to activation of a single class of chloride-channel. 2. The concentration-response curve for the peak ICl gave an apparent dissociation constant of 6.4 X 10(-5...

journal_title：British journal of pharmacology

authors： Ikemoto Y,Akaike N,Kijima H

更新日期：1988-11-01 00:00:00

abstract：:1 Physiologically, perisinusoidal hepatic stellate cells (HSC) are quiescent and store retinoids. During liver injury and in cell culture, HSC transform into proliferating myofibroblast-like cells that express alpha-smooth muscle actin (alpha-sma) and produce excessive amounts of extracellular matrix. During transform...

journal_title：British journal of pharmacology

authors： Chi X,Anselmi K,Watkins S,Gandhi CR

更新日期：2003-06-01 00:00:00

abstract：:1. [35S]t-butylbicyclophosphorothionate (TBPS) is a high affinity ligand for the picrotoxin site of GABA(A) receptors. Here we examined TBPS binding to the cloned receptors made of alpha 1, alpha 3 or alpha 6 in combination with beta 2 or beta 2 and gamma 2 subunits, in the presence of GABA and several allosteric liga...

journal_title：British journal of pharmacology

authors： Im WB,Pregenzer JF,Thomsen DR

更新日期：1994-08-01 00:00:00

abstract：:1 A 3 min intracoronary infusion of adenosine (50 mug/min) produced a significant decrease in coronary artery perfusion pressure, left ventricular systolic pressure and myocardial O2 consumption in the isolated supported heart preparation of the dog perfused at a constant coronary blood flow. Heart rate was controlled...

journal_title：British journal of pharmacology

authors： Gross GJ,Hardman HF,Warltier DC

更新日期：1976-07-01 00:00:00

abstract：:The presence of functional cannabinoid CB2 receptors in the CNS has provoked considerable controversy over the past few years. Formerly considered as an exclusively peripheral receptor, it is now accepted that it is also present in limited amounts and distinct locations in the brain of several animal species, includin...

journal_title：British journal of pharmacology

authors： Benito C,Tolón RM,Pazos MR,Núñez E,Castillo AI,Romero J

更新日期：2008-01-01 00:00:00

abstract：:1. In order to characterize the neuropeptide Y (NPY) Y1 receptors known to be present in rabbit isolated vas deferens and saphenous vein, the pharmacological activity of the selective NPY Y1 receptor agonists, [Leu31,Pro34] NPY and various other peptide agonists, together with the putative NPY antagonist, benextramine...

journal_title：British journal of pharmacology

authors： Palea S,Corsi M,Rimland JM,Trist DG

更新日期：1995-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Early soluble epoxide hydrolase inhibitors (sEHIs) such as 12-(3-adamantan-1-yl-ureido)-dodecanoic acid (AUDA) are effective anti-hypertensive and anti-inflammatory agents in various animal models. However, their poor metabolic stability and limited water solubility make them difficult to use pha...

journal_title：British journal of pharmacology

authors： Liu JY,Tsai HJ,Hwang SH,Jones PD,Morisseau C,Hammock BD

更新日期：2009-01-01 00:00:00

abstract：:1 Hypothalamic blood flow (HBF) was measured in conscious rabbits by the 133xenon washout technique. 2 Substance P in a dose of 50 or 500 ng increases HBF while 5 ng is without effect. 3 Cholinoceptor blockade, with either atropine or mecamylamine abolishes the vasodilator effect of substance P. 4 Chemical sympathecto...

journal_title：British journal of pharmacology

authors： Klugman KP,Lembeck F,Markowitz S,Mitchell G,Rosendorff C

更新日期：1980-01-01 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：:We examined whether a specific aminopeptidase P (APP) inhibitor, apstatin, increases vasodepressor responses to bradykinin in anaesthetized rats, and whether it would augment blood pressure responses further after treatment with the angiotensin-converting enzyme inhibitor (ACEi), lisinopril. Apstatin doubled the maxim...

journal_title：British journal of pharmacology

authors： Kitamura S,Carbini LA,Carretero OA,Simmons WH,Scicli AG

更新日期：1995-01-01 00:00:00

abstract：:1. We have characterized the human smooth muscle endothelin converting enzyme (ECE) present in the media of the endothelium-denuded human umbilical vein preparation. 2. Endothelin-1 (ET-1) and ET-2 were potent constrictors of umbilical vein with EC50 values of 9.2 nM and 29.6 nM, respectively. ET-1 was at least 30 tim...

journal_title：British journal of pharmacology

authors： Maguire JJ,Johnson CM,Mockridge JW,Davenport AP

更新日期：1997-12-01 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：BACKGROUND AND PURPOSE:Montelukast and S-carbocysteine have been used in asthmatic patients as an anti-inflammatory or mucolytic agent respectively. S-carbocysteine also exhibits anti-inflammatory properties. EXPERIMENTAL APPROACH:Ovalbumin (OVA) sensitized BALB/c mice were challenged with OVA for 3 days followed by s...

journal_title：British journal of pharmacology

authors： Takeda K,Shiraishi Y,Matsubara S,Miyahara N,Matsuda H,Okamoto M,Joetham A,Gelfand EW

更新日期：2010-07-01 00:00:00

abstract：:In this issue of the BJP, Green et al. suggest that animal data could not be used to predict the adverse effects of 3,4-methylenedioxymethamphetamine (MDMA) in humans and that MDMA did not produce 5-HT neurotoxicity in the human brain. This proposal was, however, not accompanied by a review of the empirical evidence i...

journal_title：British journal of pharmacology

authors： Parrott AC

更新日期：2012-07-01 00:00:00

abstract：:1 The effects of the prostaglandin synthetase inhibitor, indomethacin and the prostaglandin antagonist SC-19220 (1-acetyl-2-[8-chloro-10,11-dihydrodibenz (b,f) (1,4)oxazepine-10-carbonyl] hydrazine), were examined on the tone of the guinea-pig isolated tracheal preparation and on the responses of the preparation to pr...

journal_title：British journal of pharmacology

authors： Farmer JB,Farrar DG,Wilson J

更新日期：1974-12-01 00:00:00

abstract：:Idiopathic pulmonary fibrosis (IPF) is a fatal lung disease where the additional presence of pulmonary hypertension (PH) reduces survival. In particular, the presence of coexistent pulmonary vascular disease in patients with advanced lung parenchymal disease results in worse outcomes than either diagnosis alone. This ...

journal_title：British journal of pharmacology

authors： Rajagopal K,Bryant AJ,Sahay S,Wareing N,Zhou Y,Pandit LM,Karmouty-Quintana H

更新日期：2021-01-01 00:00:00

abstract：:Des-Arg9-bradykinin (des-Arg9-BK) caused endothelium-dependent relaxations in human, isolated coronary arteries which upregulated with in vitro incubation time. Relaxations to des-Arg9-BK were inhibited by the B1 receptor antagonist, des-Arg9-[Leu3]-BK (pK(B), 6.14 +/- 0.11) but were unaffected by the B2 receptor anta...

journal_title：British journal of pharmacology

authors： Drummond GR,Cocks TM

更新日期：1995-12-01 00:00:00

abstract：:1. A method is presented which enables the dissociation constant (KI) of a competitive, pseudo-irreversible or non-competitive antagonist-receptor complex to be estimated without knowledge of agonist concentrations. 2. The technique has been tested using sets of concentration-response data which simulated these variou...

journal_title：British journal of pharmacology

authors： Mackay D

更新日期：1994-01-01 00:00:00

abstract：:1. A synthetic oxytocin analogue, [1-N-carbamoyl-hemicystine-2-O-methyltyrosine]-oxytocin (carbamoyl-methyloxytocin), has been tested as an antagonist to the actions of oxytocin and vasopressin on the uterus, the mammary gland and blood pressure.2. The analogue inhibited the response of the isolated rat uterus to both...

journal_title：British journal of pharmacology

authors： Bisset GW,Clark BJ,Krejcí I,Polácek I,Rudinger J

更新日期：1970-10-01 00:00:00

abstract：:1. N(G)-monomethyl-L-arginine (L-NMMA) constricts human forearm resistance vasculature and selectively attenuates vasodilator responses to endothelium-dependent vasodilators. Incomplete inhibition of such responses could be due to an inadequate dose of L-NMMA or to NO-independent vasodilator mechanisms. 2. This study ...

journal_title：British journal of pharmacology

authors： Dawes M,Chowienczyk PJ,Ritter JM

更新日期：2001-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Erectile dysfunction is highly prevalent in diabetic patients and PDE V inhibitors are effective and safe for the treatment of erectile dysfunction in men with diabetes. Therefore, in this study we investigated whether a pharmacokinetic interaction occurs between DA-8159 and metformin, as both dr...

journal_title：British journal of pharmacology

authors： Choi YH,Chung SJ,Lee MG

更新日期：2008-04-01 00:00:00

abstract：:1. Adenosine has been shown to be responsible for the hyperaemic response of the hepatic artery to portal vein occlusion (the hepatic arterial 'buffer response'). 2. The effect of adenosine receptor blockade and of adenosine uptake inhibition on the hepatic arterial response to portal vein occlusion was investigated i...

journal_title：British journal of pharmacology

authors： Mathie RT,Alexander B

更新日期：1990-07-01 00:00:00

abstract：:1. Morphine-like analgesic drugs caused depression of twitches of the isolated guinea-pig ileum in response to transmural electrical stimulation. The drugs tested were the narcotic analgesics codeine, diamorphine, fentanyl, morphine, morphine-N-oxide, normorphine, oxymorphone, pethidine, phenazocine and phenoperidine ...

journal_title：British journal of pharmacology

authors： Fennessy MR,Heimans RL,Rand MJ

更新日期：1969-10-01 00:00:00

abstract：:1. A study has been made of the modulation of high-voltage activated transient and sustained calcium currents in cultured neurones of avian ciliary ganglia by nitric oxide (NO) and arachidonic acid. 2. Sodium nitroprusside (100 microM) reduced the transient calcium current (ICa) on average by 31% and the sustained ICa...

journal_title：British journal of pharmacology

authors： Khurana G,Bennett MR

更新日期：1993-06-01 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：:In moderate-to-severe asthma, adding an inhaled long-acting β2 -adenoceptor agonist (LABA) to an inhaled corticosteroid (ICS) provides better disease control than simply increasing the dose of ICS. Acting on the glucocorticoid receptor (GR, gene NR3C1), ICSs promote anti-inflammatory/anti-asthma gene expression. In vi...

journal_title：British journal of pharmacology

authors： Newton R,Giembycz MA

更新日期：2016-12-01 00:00:00