Pharmacokinetic-pharmacodynamic modelling of the anti-lipolytic and anti-ketotic effects of the adenosine A1-receptor agonist N6-(p-sulphophenyl)adenosine in rats.

abstract：BACKGROUND AND PURPOSE:Following transient focal stroke, rapid accumulation and activation of neutrophils in the ischaemic region is deleterious due to release of reactive oxygen species and myeloperoxidase (MPO). The purpose of this study was to examine whether AM-36, both a Na+ channel blocker and an antioxidant, aff...

journal_title：British journal of pharmacology

authors： Weston RM,Jarrott B,Ishizuka Y,Callaway JK

更新日期：2006-11-01 00:00:00

abstract：:1. The effects of the nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME) on vasoconstrictor responses to transmural electrical nerve stimulation and noradrenaline were examined in the rabbit isolated renal artery with and without an intact endothelium. In addition, the effect of removing the end...

journal_title：British journal of pharmacology

authors： Vials AJ,Crowe R,Burnstock G

更新日期：1997-05-01 00:00:00

abstract：:1. Ezetimibe potently inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. The effect of ezetimibe on known absorptive processes was determined in the present studies. 2. Experiments were conducted in the hamster and...

journal_title：British journal of pharmacology

authors： van Heek M,Farley C,Compton DS,Hoos L,Davis HR

更新日期：2001-09-01 00:00:00

abstract：:1. In the present paper, we describe the in vitro pharmacological properties of LF 16.0335 (1-[[3-[(2,4-dimethylquinolin-8-yl)oxymethyl]-2,4-dichloro-p henyl]sulphonyl] -2(S) - [[4 -[4-(aminoiminomethyl)phenylcarbonyl]piperazin-1-yl]ca rbonyl]pyrrolidine), a novel and potent nonpeptide antagonist of the human bradykin...

journal_title：British journal of pharmacology

authors： Pruneau D,Luccarini JM,Fouchet C,Defrêne E,Franck RM,Loillier B,Duclos H,Robert C,Cremers B,Bélichard P,Paquet JL

更新日期：1998-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The rat respiratory muscle diaphragm has markedly lower sensitivity than the locomotor muscle extensor digitorum longus (EDL) to the new acetylcholinesterase (AChE) inhibitors, alkylammonium derivatives of 6-methyluracil (ADEMS). This study evaluated several possible reasons for differing sensiti...

journal_title：British journal of pharmacology

authors： Petrov KA,Yagodina LO,Valeeva GR,Lannik NI,Nikitashina AD,Rizvanov AA,Zobov VV,Bukharaeva EA,Reznik VS,Nikolsky EE,Vyskočil F

更新日期：2011-06-01 00:00:00

abstract：:1 ATP is an important vasoactive mediator, which acts via two receptor classes: P2X and P2Y. Activation of P2X receptors has traditionally been associated with the well-characterised vasoconstrictor properties of ATP. 2 In the current study, we have shown that the P2X(1 & 3) receptor ligand, alpha, beta methylene ATP,...

journal_title：British journal of pharmacology

authors： Harrington LS,Mitchell JA

更新日期：2004-11-01 00:00:00

abstract：:1. The pathological features of Gram-positive shock can be mimicked by the co-administration of two cell wall components of Staphylococcus aureus, namely lipoteichoic acid (LTA) and peptidoglycan (PepG). This is associated with the expression of the inducible isoform of nitric oxide synthase (iNOS) in various organs. ...

journal_title：British journal of pharmacology

authors： Kengatharan KM,De Kimpe SJ,Thiemermann C

更新日期：1996-12-01 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：:1 In the isolated basilar artery of the rabbit, gamma-aminobutyrate acid (GABA) (ED50 +/- s.e. mean, 2.4 +/- 1.1 x 10(-5) M) produced a relaxation, if the tone had been increased with 5-hydroxytryptamine (5-HT). 2 3-Aminoproprane sulphonic acid (3-APS) produced a similar, but smaller relaxation, while baclofen had no ...

journal_title：British journal of pharmacology

authors： Anwar N,Mason DF

更新日期：1982-01-01 00:00:00

abstract：:The hypothesis of negative feedback regulation of noradrenaline release was studied in guinea-pig left atrial halves mounted in vitro. Tissues were transmurally stimulated with 30, 100 or 300 pulses at 2 Hz with pulse durations ranging from 50 mus to 2,000 mus, and the efflux of 3H-transmitter determined. The efflux o...

journal_title：British journal of pharmacology

authors： Kalsner S

更新日期：1983-08-01 00:00:00

abstract：:1. Previous studies demonstrated that elevation of the extracellular calcium concentration during a prolonged exposure to a high concentration of carbachol reverses the staurosporine-induced decrease in the extent of endplate resensitization in voltage-clamped snake twitch fibres. The present studies were designed to ...

journal_title：British journal of pharmacology

authors： Hardwick JC,Parsons RL

更新日期：1993-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Xaliproden (SR57746A) is a 5-HT(1A) receptor agonist and neurotrophic agent that reduces oxaliplatin-mediated neuropathy in clinical trials. The present study investigated its profile on in vitro transduction, neurochemical responses and acute nociceptive pain tests in rats. EXPERIMENTAL APPROAC...

journal_title：British journal of pharmacology

authors： Martel JC,Assié MB,Bardin L,Depoortère R,Cussac D,Newman-Tancredi A

更新日期：2009-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:QT prolongation is commonly used as a surrogate marker for Torsade de Pointes (TdP) risk of non-cardiovascular drugs. However, use of this indirect marker often leads to misinterpretation of the realistic TdP risk, as tested compounds may cause QT prolongation without evoking TdP in humans. A neg...

journal_title：British journal of pharmacology

authors： Guns PJ,Johnson DM,Van Op den Bosch J,Weltens E,Lissens J

更新日期：2012-05-01 00:00:00

abstract：:Two-state and operational models of both agonism and allosterism are compared to identify and characterize common pharmacological parameters. To account for the receptor-dependent basal response, constitutive receptor activity is considered in the operational models. By arranging two-state models as the fraction of ac...

journal_title：British journal of pharmacology

authors： Roche D,Gil D,Giraldo J

更新日期：2013-07-01 00:00:00

abstract：:3,4-Methylenedioxymethamphetamine (MDMA, 'ecstasy') administration to rats produces hyperthermia if they are housed in normal or warm ambient room temperature (Ta) conditions (>or=20 degrees C), but hypothermia when in cool conditions (Ta

journal_title：British journal of pharmacology

authors： Green AR,O'Shea E,Saadat KS,Elliott JM,Colado MI

更新日期：2005-09-01 00:00:00

abstract：:1. Patients with airway infection by Pseudomonas aeruginosa have impaired mucociliary clearance. Pyocyanin is a phenazine pigment produced by P. aeruginosa which is present in the sputum of colonized patients, slows human ciliary beat frequency (CBF) in vitro and slows mucociliary transport in vivo in the guinea-pig. ...

journal_title：British journal of pharmacology

authors： Kanthakumar K,Cundell DR,Johnson M,Wills PJ,Taylor GW,Cole PJ,Wilson R

更新日期：1994-06-01 00:00:00

abstract：:1. A grease-gap technique has been used to measure d.c. potentials, in response to the application of excitatory amino acids and electrical stimulation of the Schaffer collateral-commissural pathway, in the CA1 region of rat hippocampal slices. The actions of L-glutamate (L-Glu) have been quantified and compared to th...

journal_title：British journal of pharmacology

authors： Frenguelli BG,Blake JF,Brown MW,Collingridge GL

更新日期：1991-02-01 00:00:00

abstract：:1. The effects of melanotrophin release inhibiting factor (MIF) and its cyclic analogue cyclo (Leu-Gly) on tolerance to the analgesic effect of morphine were studied in male Sprague-Dawley rats. 2. Tolerance to morphine was induced by implantation of four morphine pellets (each containing 75 mg of morphine free base) ...

journal_title：British journal of pharmacology

authors： Bhargava HN

更新日期：1981-04-01 00:00:00

abstract：:Ginsenoside Rg1, an active ingredient in ginseng, was previously shown to be a novel class of potent phytoestrogen. The present study aims at investigating the molecular mechanisms involved in mediating its actions in human breast cancer (MCF-7) cells. Rg1 (1 pM) stimulates cell proliferation (P<0.01) and estrogen-res...

journal_title：British journal of pharmacology

authors： Chen WF,Lau WS,Cheung PY,Guo DA,Wong MS

更新日期：2006-03-01 00:00:00

abstract：:Multiple myeloma is a neoplastic disorder of plasma cells characterized by clonal proliferation within the bone marrow. One of the major clinical features of multiple myeloma is the destructive osteolytic bone disease that occurs in the majority of patients. Myeloma bone disease is associated with increased osteoclast...

journal_title：British journal of pharmacology

authors： Webb SL,Edwards CM

更新日期：2014-08-01 00:00:00

abstract：:By examination of compound action potentials in the saphenous nerve of the anaesthetized rat it has been shown that capsaicin causes a rapid, dose-dependent, failure of conduction in many C-fibres when applied directly to the nerve. A large reduction in C-fibre conduction occurs with concentrations as low as 110 micro...

journal_title：British journal of pharmacology

authors： Baranowski R,Lynn B,Pini A

更新日期：1986-10-01 00:00:00

abstract：:1. In order to investigate the modulatory effects of adenosine on excitatory amino acid projections onto striatal medium spiny neurons, whole-cell patch clamp experiments were carried out in rat brain slices. The effects of various agonists for P1 (adenosine) and P2 (ATP) purinoceptors and their antagonists were inves...

journal_title：British journal of pharmacology

authors： Nörenberg W,Wirkner K,Illes P

更新日期：1997-09-01 00:00:00

abstract：:The distribution of beta-adrenoceptor subtypes in slide-mounted sections of guinea-pig kidney has been examined by the technique of in vitro labelling combined with autoradiography. Binding of (-)-[125I]-cyanopindolol (Cyp) to kidney sections equilibrated and dissociated slowly, was saturable and stereoselective with ...

journal_title：British journal of pharmacology

authors： Lew R,Summers RJ

更新日期：1985-06-01 00:00:00

abstract：:1 Prolonged exposure (6-12 h) of rat aorta to alpha1-adrenergic receptor (alpha(1)AR) agonist phenylephrine (Phe) leads to a decrease in alpha(1)AR-mediated vasoconstriction. This reduced responsiveness to alpha(1)AR stimulation was strongly dependent on the intactness of the endothelium. 2 We examined the effect of P...

journal_title：British journal of pharmacology

authors： Gürdal H,Can A,Uğur M

更新日期：2005-05-01 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 Human luteal tissue slices from days 18, 21 and 25 of the menstrual cycle were superfused in vitro with Medium 199 alone or containing cloprostenol (1 microgram/ml). Concentrations of progesterone, oestradiol-17beta and prostaglandins F2alpha and E2 were determined in the superfusate samples. 2 Secretion of steroids...

journal_title：British journal of pharmacology

authors： McDougall AN,Walker FM,Watson J

更新日期：1977-07-01 00:00:00

abstract：:The oestrogenic and antioestrogenic activities of a series of substituted derivatives of 1,1,2 triphenylbut-1-ene have been determined using primary cultures of rat pituitary gland cells to monitor prolactin synthesis in vitro. The relative binding affinity of the agonists for the oestrogen receptor was consistent wit...

journal_title：British journal of pharmacology

authors： Jordan VC,Koch R,Mittal S,Schneider MR

更新日期：1986-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Volume-regulated anion channels (VRACs) play an important role in cell-volume regulation. alpha(1)-Adrenoceptor stimulation by phenylephrine (PE) suppressed the hypotonic activation of VRAC current in mouse ventricular cells and regulatory volume decrease (RVD) was also absent in PE-treated cells...

journal_title：British journal of pharmacology

authors： Ichishima K,Yamamoto S,Iwamoto T,Ehara T

更新日期：2010-09-01 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：: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