A kinetic study on the stereospecific inhibition of KCNQ1 and I(Ks) by the chromanol 293B.

abstract：:1 Nateglinide, a novel oral hypoglycemic agent, rapidly reaches the maximum serum concentration after oral administration, suggesting that it is rapidly absorbed in the gastrointestinal tract. The aim of this work is to clarify the intestinal absorption mechanism of nateglinide by means of in vitro studies. 2 We exami...

journal_title：British journal of pharmacology

authors： Okamura A,Emoto A,Koyabu N,Ohtani H,Sawada Y

更新日期：2002-10-01 00:00:00

abstract：:1. This study investigated the importance of renal sympathetic nerves in regulating sodium and water excretion from the kidneys of stroke prone spontaneously hypertensive and 2K1C Goldblatt hypertensive rats anaesthetized with chloralose/urethane (17.5/300 mg initially and supplemented at regular intervals), and prepa...

journal_title：British journal of pharmacology

authors： Chamienia AL,Johns EJ

更新日期：1996-08-01 00:00:00

abstract：:1. 5-Hydroxytryptamine (5-HT) is known to produce a number of different effects in the gastrointestinal tract of various species, and has been proposed to play a key role in a number of intestinal disorders in man, including irritable bowel syndrome (IBS), although the receptors involved have yet to be established. Th...

journal_title：British journal of pharmacology

authors： Borman RA,Tilford NS,Harmer DW,Day N,Ellis ES,Sheldrick RL,Carey J,Coleman RA,Baxter GS

更新日期：2002-03-01 00:00:00

abstract：:1. Our study was aimed at investigating the duration of the bronchodilator action of the antimuscarinc drug glycopyrrolate compared to tiotropium and ipratropium. In the guinea-pig isolated trachea, the time (t1/2) necessary for a contractile response to carbachol (0.3 microM) to return to 50% recovery after washout o...

journal_title：British journal of pharmacology

authors： Villetti G,Bergamaschi M,Bassani F,Bolzoni PT,Harrison S,Gigli PM,Janni A,Geppetti P,Civelli M,Patacchini R

更新日期：2006-06-01 00:00:00

abstract：:1. Therapeutic doses of colistin sulphomethate sodium B.P. (Colomycin), pento-N sulphomethylpolymyxin B sodium (Thiosporin) and ampicillin B.P. (Penbritin) as well as normal saline have been given to volunteers with normal kidney function.2. A blind crossover technique was used and the effects of the compounds on bloo...

journal_title：British journal of pharmacology

authors： Caldwell AD,Martin AJ,Trigger DJ

更新日期：1969-09-01 00:00:00

abstract：:The electrically-evoked contractions of the rat vas deferens were selectively inhibited by beta-endorphin, the preparation being much less sensitive to enkephalins and narcotic analgesic drugs. However, introduction of D-Ala in position 2 of [Leu]-enkephalin enhanced the activity of the opioid peptide to the order of ...

journal_title：British journal of pharmacology

authors： Lemaire S,Magnan J,Regoli D

更新日期：1978-11-01 00:00:00

abstract：:The role of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) in the upper urinary tract of the guinea-pig and rat was examined using simultaneous tension recordings of the proximal and distal regions of the renal pelvis and the ureter. The guinea-pig upper urinary tract contracted at a frequency (7.52+/-0.3 min...

journal_title：British journal of pharmacology

authors： Davidson ME,Lang RJ

更新日期：2000-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibitors of phosphodiesterase 5 (PDE5) affect signalling pathways by elevating cGMP, which is a second messenger involved in processes of neuroplasticity. In the present study, the effects of the PDE5 inhibitor, sildenafil, on the pathological features of Alzheimer's disease and on memory-relat...

journal_title：British journal of pharmacology

authors： Cuadrado-Tejedor M,Hervias I,Ricobaraza A,Puerta E,Pérez-Roldán JM,García-Barroso C,Franco R,Aguirre N,García-Osta A

更新日期：2011-12-01 00:00:00

abstract：:1. The present study addressed the role of neuropeptide (NPY) Y2 receptors in neurogenic contraction of mesenteric resistance arteries from female spontaneously hypertensive rats (SHR). Arteries were suspended in microvascular myographs, electrical field stimulation (EFS) was performed, and protein evaluated by Wester...

journal_title：British journal of pharmacology

authors： Gradin KA,Buus CL,Li JY,Frøbert O,Simonsen U

更新日期：2006-07-01 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：:1. We aimed to determine whether nitric oxide (NO) and/or the endothelium is involved in cholinergic neurogenic vasodilatation in the rat isolated hindquarters. 2. The abdominal aorta was cannulated for perfusion of the rat hindquarters with Krebs bicarbonate solution containing phenylephrine, to induce basal constric...

journal_title：British journal of pharmacology

authors： Loke KE,Sobey CG,Dusting GJ,Woodman OL

更新日期：1994-06-01 00:00:00

abstract：:1. SCA40 (1nM-10 microM), isoprenaline (1-300 nM) and levcromakalim (100 nM-10 microM) each produced concentration-dependent suppression of the spontaneous tone of guinea-pig isolated trachea. Propranolol (1 microM) markedly (approximately 150 fold) antagonized isoprenaline but did not antagonize SCA40. The tracheal r...

journal_title：British journal of pharmacology

authors： Cook SJ,Archer K,Martin A,Buchheit KH,Fozard JR,Müller T,Miller AJ,Elliott KR,Foster RW,Small RC

更新日期：1995-01-01 00:00:00

abstract：:AMPA-type glutamate receptors are one of the most dynamic components of excitatory synapses. Their regulated addition and removal from synapses leads to long-lasting forms of synaptic plasticity, known as long-term potentiation (LTP) and long-term depression (LTD). In addition, AMPA receptors reach their synaptic targ...

journal_title：British journal of pharmacology

authors： Esteban JA

更新日期：2008-03-01 00:00:00

abstract：:1. In response to pancreatic injury and in cell culture, pancreatic stellate cells (PSCs) are transformed ('activated') into highly proliferative myofibroblast-like cells, which express alpha-smooth muscle actin (alpha-SMA), and produce type I collagen and other extracellular matrix components. There is accumulating e...

journal_title：British journal of pharmacology

authors： Masamune A,Kikuta K,Satoh M,Satoh K,Shimosegawa T

更新日期：2003-12-01 00:00:00

abstract：:1. Besides its antimuscarinic effects, propiverine may possess an additional mode of action. We compared the effects of propiverine, three of its metabolites (M-5, M-6, M-14) and atropine in human, pig and mouse urinary bladder preparations in order to elucidate the nature of a possible additional mode of action. 2. L...

journal_title：British journal of pharmacology

authors： Wuest M,Hecht J,Christ T,Braeter M,Schoeberl C,Hakenberg OW,Wirth MP,Ravens U

更新日期：2005-07-01 00:00:00

abstract：:Ligands targeting GPCRs can be categorized according to their intrinsic efficacy to trigger a specific, receptor-mediated response. A ligand endowed with the same level of efficacy as the endogenous agonist can be classified as a full agonist, whereas a compound that displays greater efficacy, that is, higher receptor...

journal_title：British journal of pharmacology

authors： Schrage R,De Min A,Hochheiser K,Kostenis E,Mohr K

更新日期：2016-10-01 00:00:00

abstract：:Athletes attempt to improve performance with drugs that act on the beta-adrenergic system directly or indirectly. Of three beta-adrenoceptor (AR) subtypes, the beta(2)-AR is the main target in sport; they have bronchodilator and anabolic actions and enhance anti-inflammatory actions of corticosteroids. Although demons...

journal_title：British journal of pharmacology

authors： Davis E,Loiacono R,Summers RJ

更新日期：2008-06-01 00:00:00

abstract：:1 The intravenous infusion of isoprenaline and salbutamol into the greyhound increased heart rate and levels of free fatty acids, lactic acid and glucose. 2 On terminating the infusions of isoprenaline the changes produced declined rapidly but the effects produced by salbutamol were more persistent. When high doses of...

journal_title：British journal of pharmacology

authors： Kelly JG,Shanks RG

更新日期：1975-02-01 00:00:00

abstract：:1. Piperazinylindoles (DPI 201-106, BDF 8784), drugs known to act on voltage-dependent Na(+)-channels, bind with very high affinity to a Ca2(+)-channel-associated phenylalkylamine receptor in Drosophila melanogaster head membranes. These compounds and (+)-tetrandrine, a naturally occurring Ca2(+)-antagonist, were the ...

journal_title：British journal of pharmacology

authors： Glossmann H,Zech C,Striessnig J,Staudinger R,Hall L,Greenberg R,Armah BI

更新日期：1991-02-01 00:00:00

abstract：:Arthritis-associated inflammatory pain represents a serious medical problem worldwide. Current treatments for arthritic pain are not very effective and cause unwanted side effects. Resolvins, including the resolvin D and resolvin E series, are a family of novel endogenous lipid mediators derived from ω-3 polyunsaturat...

journal_title：British journal of pharmacology

authors： Xu ZZ,Ji RR

更新日期：2011-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:To determine whether there is an association between vascular NADPH oxidase (NOX), superoxide, the small GTPase Rac(1) and PDE type 5 (PDE5) in human vascular smooth muscle cell (hVSMCs). EXPERIMENTAL APPROACH:hVSMCs were incubated with xanthine-xanthine oxidase (X-XO; a superoxide generating sy...

journal_title：British journal of pharmacology

authors： Muzaffar S,Shukla N,Bond M,Sala-Newby GB,Newby AC,Angelini GD,Jeremy JY

更新日期：2008-11-01 00:00:00

abstract：:1. We have investigated the effects of salmeterol (0.3-50 microM) on several pro-inflammatory activities of human neutrophils in vitro. 2. Oxidant production by FMLP- and calcium ionophore (A23187)-activated neutrophils was particularly sensitive to inhibition by low concentrations (0.3-3 microM) of salmeterol, while ...

journal_title：British journal of pharmacology

authors： Anderson R,Feldman C,Theron AJ,Ramafi G,Cole PJ,Wilson R

更新日期：1996-04-01 00:00:00

abstract：:1. The presence of an endogenous digitalis-like factor (EDLF) in the plasma of both normal and volume expanded animals is well documented. In this study we have used ouabain and bufalin as pharmacological analogues to mimic the renal effects of EDLF and to investigate whether any interaction occurs between atrial natr...

journal_title：British journal of pharmacology

authors： Yates NA,McDougall JG

更新日期：1993-03-01 00:00:00

abstract：:The response to vasoactive agents of microvessels of the rat was tested in vivo by direct microscopic observation of the exteriorized mesentery and assessment of cutaneous vascular permeability changes with Evans blue. The constrictor response to a standard amount of noradrenaline in mesenteric microvessels was fully ...

journal_title：British journal of pharmacology

authors： Fortes ZB,Garcia Leme J,Scivoletto R

更新日期：1984-11-01 00:00:00

abstract：:Rabbits treated with 2-deoxy-D-glucose (2DG) (300 mg/kg) show an increased intake of food and water. Pretreatment with haloperidol (1 mg/kg) abolishes the increase in water intake but does not prevent the increase in food intake. ...

journal_title：British journal of pharmacology

authors： Anderson J,Sharman DF,Stephens DB

更新日期：1979-05-01 00:00:00

abstract：:In this issue MacMillan and McCarron in 2010 demonstrated that the phospholipase C (PLC) inhibitor U-73122 can potently inhibit Ca(2+) release from isolated smooth muscle cells independent of its effect on PLC. Their data suggest that the PLC inhibitor can block the sarcoplasmic/endoplasmic reticulum calcium ATPase pu...

journal_title：British journal of pharmacology

authors： Hollywood MA,Sergeant GP,Thornbury KD,McHale NG

更新日期：2010-07-01 00:00:00

abstract：:1. We have investigated the effects of a standardised mixture of hydroxyethylrutosides (HR, Venoruton), a mixture of five of its main components (M) and each of the five components separately (7-mono-HR, 7,4'-di-HR, 7,3',4'-tri-HR, 5,7,3',4'-tetra-HR and 7,3'4'-tri HQ) upon the permeability of single perfused capillar...

journal_title：British journal of pharmacology

authors： Kendall S,Towart R,Michel CC

更新日期：1993-09-01 00:00:00

abstract：:1. It has recently been shown that both alpha(1)- and alpha(2)-adrenoceptors mediate vasoconstriction in the canine external carotid circulation. The present study set out to identify the specific subtypes (alpha(1A), alpha(1B) and alpha(1D) as well as alpha(2A), alpha(2B) and alpha(2C)) mediating the above response. ...

journal_title：British journal of pharmacology

authors： Willems EW,Valdivia LF,Saxena PR,Villalón CM

更新日期：2001-03-01 00:00:00

abstract：:1. This study examined the impact of allopurinol on the renal functional responses to a 30 min period of ischaemia in anaesthetized rats. 2. Immediately on reperfusion, blood pressure rose transiently, while renal blood flow remained stable throughout at control values. Glomerular filtration rate was decreased by some...

journal_title：British journal of pharmacology

authors： Hestin D,Johns EJ

更新日期：1999-09-01 00:00:00

abstract：:1. The signal transduction pathway for vasorelaxation induced by human alpha-calcitonin gene-related peptide (human alpha-CGRP) was studied in rat thoracic aortic rings preconstricted with noradrenaline (10(-7) M). 2. Vasorelaxation by human alpha-CGRP was inhibited by haemoglobin (10(-6) M) and methylene blue (10(-5)...

journal_title：British journal of pharmacology

authors： Gray DW,Marshall I

更新日期：1992-11-01 00:00:00