Retracted: Addition of a single methyl group to a small molecule sodium channel inhibitor introduces a new mode of gating modulation, by L Wang, SG Zellmer, DM Printzenhoff and NA Castle. British Journal of Pharmacology, volume 172(20): 4905-4918, publish

abstract：:1. By use of the whole-cell configuration of the patch-clamp technique, membrane currents induced by cyclopiazonic acid (CPA; an inhibitor of the sarcoplasmic reticulum (SR) calcium-ATPase) were investigated in single smooth muscle cells freshly dispersed from the mouse anococcygeus. Voltage-dependent calcium currents...

journal_title：British journal of pharmacology

authors： Wayman CP,McFadzean I,Gibson A,Tucker JF

更新日期：1996-02-01 00:00:00

abstract：:1. This study was designed to assess the molecular and cellular events involved in the up-regulation (and receptor supersensitivity) of brain alpha(2)-adrenoceptors as a result of chronic depletion of noradrenaline (and other monoamines) by reserpine. 2. Chronic reserpine (0.25 mg kg(-1) s.c., every 48 h for 6 - 14 da...

journal_title：British journal of pharmacology

authors： Ribas C,Miralles A,Busquets X,García-Sevilla JA

更新日期：2001-04-01 00:00:00

abstract：:1. The effects of palytoxin (PTX) isolated from Palythoa tubercurosa were tested on the isolated intra-arterially perfused spinal cord of the frog. The resting and evoked potentials were recorded by means of a sucrose-gap technique. 2. PTX caused a marked depolarization of both ventral and dorsal roots. The minimum ef...

journal_title：British journal of pharmacology

authors： Kudo Y,Shibata S

更新日期：1980-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibition of the T- and B-cell interaction through the CD40/CD40 ligand (L) axis is a favourable approach for inflammatory disease treatment. Clinical studies of anti-CD40L molecules in autoimmune diseases have met challenges because of thromboembolic events and adverse haemostasis. VIB4920 (for...

journal_title：British journal of pharmacology

authors： Nicholson SM,Casey KA,Gunsior M,Drabic S,Iverson W,Cook H,Scott S,O'Day T,Karanth S,Dixit R,Ryan PC

更新日期：2020-03-01 00:00:00

abstract：:1. The effect of the nitro-derivative of aspirin, NCX4016, was assessed on ischaemic ventricular arrhythmias and myocardial infarct size in anaesthetized pigs in comparison to native aspirin. 2. Pigs were given aspirin (10 mg kg(-1); n=6), low dose NCX4016 (18.4 mg kg(-1); n=6) or high dose NCX4016 (60 mg kg(-1); n=7)...

journal_title：British journal of pharmacology

authors： Wainwright CL,Miller AM,Work LM,Del Soldato P

更新日期：2002-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Rosiglitazone is an anti-diabetic drug improving insulin sensitivity and glucose uptake in skeletal muscle and adipose tissues. However, several recent clinical trials suggest that rosiglitazone can increase the risk of cardiovascular ischaemia, although other studies failed to show such risks. T...

journal_title：British journal of pharmacology

authors： Yu L,Jin X,Yang Y,Cui N,Jiang C

更新日期：2011-12-01 00:00:00

abstract：:1. The electrical activity of guinea-pig pelvic ganglion cells following iontophoretically applied cholinergic drugs, alone and during orthodromic nerve stimulation via the hypogastric nerve, has been recorded intracellularly.2. Iontophoretic application of nicotine (Nic) and acetylcholine (ACh) reduced membrane resis...

journal_title：British journal of pharmacology

authors： Holman ME,Muir TC,Szurszewski JH,Yonemura K

更新日期：1971-01-01 00:00:00

abstract：:In helical strips cut from the small mesenteric artery of guinea-pig (GPSMA) (0.3-0.6 mm o.d.) relaxations induced by substance P were more susceptible to damage of the endothelium by rubbing than were relaxations evoked by carbachol. Relaxations induced by 2-nicotin-amidoethyl nitrate (SG75) were unaffected by this p...

journal_title：British journal of pharmacology

authors： Bolton TB,Clapp LH

更新日期：1986-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Diabetes mellitus is associated with a specific cardiomyopathy. We compared the cardioprotective effects of an endothelin-A receptor blocker (ET(A)-RB) with those of an angiotensin-converting enzyme inhibitor (ACE-I) in rats with streptozotocin (STZ)-induced diabetes. EXPERIMENTAL APPROACH:Diabe...

journal_title：British journal of pharmacology

authors： Wölkart G,Pang X,Stessel H,Kirchengast M,Brunner F

更新日期：2007-08-01 00:00:00

abstract：:1. The chemically novel acetohydroxamic acids, BW A4C, BW A137C and BW A797C, are potent inhibitors of the synthesis of leukotriene B4 (LTB4) from arachidonic acid by human leucocyte homogenates: the concentrations required for 50% inhibition (IC50) were 0.1 microM, 0.8 microM and 0.5 microM respectively. Inhibition w...

journal_title：British journal of pharmacology

authors： Tateson JE,Randall RW,Reynolds CH,Jackson WP,Bhattacherjee P,Salmon JA,Garland LG

更新日期：1988-06-01 00:00:00

abstract：:1. Ca2+ buffering function of sarcoplasmic reticulum (SR) in the resting state of arteries from spontaneously hypertensive rats (SHR) was examined. Differences in the effects of cyclopiazonic acid (CPA) and thapsigargin, agents which inhibit the Ca(2+)-ATPase of SR, on tension and cellular Ca2+ level were assessed in ...

journal_title：British journal of pharmacology

authors： Nomura Y,Asano M,Ito K,Uyama Y,Imaizumi Y,Watanabe M

更新日期：1997-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

journal_title：British journal of pharmacology

authors： Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

更新日期：2015-09-01 00:00:00

abstract：:1. The aim of the study was to compare the effects of 14 day subcutaneous infusion of the 5-HT(2C) receptor agonists, m-chlorophenylpiperazine (mCPP, 12 mg kg(-1) day(-1)) and Ro 60-0175 (36 mg kg(-1) day(-1)) and the 5-HT releasing agent and re-uptake inhibitor, d-fenfluramine (6 mg kg(-1) day(-1)), on food and water...

journal_title：British journal of pharmacology

authors： Vickers SP,Benwell KR,Porter RH,Bickerdike MJ,Kennett GA,Dourish CT

更新日期：2000-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tumour cell migration and adhesion constitute essential features of metastasis. G-protein coupled receptor 55 (GPR55), a lysophospholipid receptor, has been shown to play an important role in carcinogenesis. Here, we investigated the involvement of GPR55 in migration and metastasis of colon cance...

journal_title：British journal of pharmacology

authors： Kargl J,Andersen L,Hasenöhrl C,Feuersinger D,Stančić A,Fauland A,Magnes C,El-Heliebi A,Lax S,Uranitsch S,Haybaeck J,Heinemann A,Schicho R

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:N-docosahexaenoylethanolamine (DHEA) is the ethanolamine conjugate of the long-chain polyunsaturated n-3 fatty acid docosahexaenoic (DHA; 22: 6n-3). Its concentration in animal tissues and human plasma increases when diets rich in fish or krill oil are consumed. DHEA displays anti-inflammatory pr...

journal_title：British journal of pharmacology

authors： Meijerink J,Poland M,Balvers MG,Plastina P,Lute C,Dwarkasing J,van Norren K,Witkamp RF

更新日期：2015-01-01 00:00:00

abstract：:1. In circular muscle strips of the fundus and corpus of guinea-pig stomach, mechanical responses to catecholamines were studied mainly in the presence of a prostaglandin biosynthesis inhibitor, meclofenamate. 2. Normal preparations developed considerable muscle tone, and adrenaline (10-100 microM) in the presence of ...

journal_title：British journal of pharmacology

authors： Syed MM,Parekh AB,Tomita T

更新日期：1990-12-01 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. The influence of different holding potentials (-120 to -70 mV) on the contraction of enzymatically dispersed myocytes from guinea-pig hearts was evaluated. Contractions were elicited by repetitive depolarizations to 0 mV at 0.5 Hz. 2. While ineffective at 140 and 5 mmol l-1 [Na+]o and pipette Na+, respectively, dep...

journal_title：British journal of pharmacology

authors： Mermi J,Yajima M,Ebner F

更新日期：1991-11-01 00:00:00

abstract：:1. Simultaneous computer modelling of control and guanfacine-masked [3H]-MK 912 saturation curves as well as guanfacine competition curves revealed that the drugs bound to two alpha 2-adrenoceptor subtypes in the rat cerebral cortex with very different selectivities. These alpha 2-adrenoceptor subtypes were designated...

journal_title：British journal of pharmacology

authors： Uhlén S,Xia Y,Chhajlani V,Felder CC,Wikberg JE

更新日期：1992-08-01 00:00:00

abstract：:The study investigated the role of endothelin (ET) and the ET receptor subtypes ET(A) and ET(B) in mediating longitudinal contraction in the mouse proximal and distal colon. Cumulative concentration-response curves to a range of ET agonists (ET-1, ET-2, ET-3, (Ala(1,3,11,13)) ET and IRL 1620) were established by admin...

journal_title：British journal of pharmacology

authors： Khan H,Naylor RJ,Tuladhar BR

更新日期：2006-03-01 00:00:00

abstract：:1. Optimal dipeptide and peptidomimetic drug transport across the intestinal mucosal surface is dependent upon the co-operative functional activity of the di/tripeptide transporter hPepT1 and the Na(+)/H(+) exchanger NHE3. The ability of the anti-absorptive enteric neuropeptide VIP (vasoactive intestinal peptide) to m...

journal_title：British journal of pharmacology

authors： Anderson CM,Mendoza ME,Kennedy DJ,Raldua D,Thwaites DT

更新日期：2003-02-01 00:00:00

abstract：:An investigation of the effects of gamma-aminobutyric acid (GABA) and the selective GABAB receptor agonist, baclofen, on basal and stimulated adenosine 3':5'-cyclic monophosphate (cyclic AMP) levels in slices of rat cerebral cortex has been carried out. Neither GABA nor baclofen produced any significant change in basa...

journal_title：British journal of pharmacology

authors： Hill DR

更新日期：1985-01-01 00:00:00

abstract：:1. NaF (10 mM) produced a 2-3 fold increase in adenylate cyclase activity in homogenates of NG108-15 cells incubated in the presence of 1 microM GTP. Higher concentrations of NaF suppressed adenylate cyclase activity. 2. In the presence of the adenosine receptor agonist 5'-(N-ethyl)-carboxamidoadenosine (NECA; 100 mic...

journal_title：British journal of pharmacology

authors： Kelly E,Keen M,Nobbs P,MacDermot J

更新日期：1990-06-01 00:00:00

abstract：:1. The actions of bretylium tosylate on neuromuscular transmission in the rat phrenic nerve diaphragm preparation have been investigated by electro-2. On the guinea-pig ileum, threshold doses elicit repeated maximal spike contractions which are blocked by atropine. In the presence of atropine, higher concentrations of...

journal_title：British journal of pharmacology

authors： Clineschmidt BV,Geller RG,Govier WC,Pisano JJ,Tanimura T

更新日期：1971-04-01 00:00:00

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. Acetylcholine mustard (N-2-chloroethyl-N-methyl-2-acetoxyethylamine), a potent muscarinic agonist, binds virtually irreversibly to muscarinic receptors in longitudinal muscle strips from guinea-pig small intesting, as shown by the inhibition of the binding of E13-H]-propylbenzilycholine mustard ([3-H-PrBCM), an aff...

journal_title：British journal of pharmacology

authors： Robinson DA,Taylor JG,Young JM

更新日期：1975-03-01 00:00:00

abstract：:Adrenomedullin (AM) has two known receptors formed by the calcitonin receptor-like receptor (CL) and receptor activity-modifying protein (RAMP) 2 or 3: we report the effects of the antagonist fragments of human AM and CGRP (AM22-52 and CGRP8-37) in inhibiting AM at human (h), rat (r) and mixed species CL/RAMP2 and CL/...

journal_title：British journal of pharmacology

authors： Hay DL,Howitt SG,Conner AC,Schindler M,Smith DM,Poyner DR

更新日期：2003-10-01 00:00:00

abstract：:1. We have used the whole-cell patch clamp technique to study the effect of the partial anti-oestrogens clomiphene and nafoxidine, the pure anti-oestrogens ICI 182,780 and RU 58,668 and the oestrogen ss-estradiol, on the volume-regulated anion channel (VRAC) in cultured pulmonary artery endothelial (CPAE) cells. 2. In...

journal_title：British journal of pharmacology

authors： Maertens C,Droogmans G,Chakraborty P,Nilius B

更新日期：2001-01-01 00:00:00

abstract：:1. The effects of dimethothiazine have been studied on the response of afferent fibres from primary and secondary endings of muscle spindles in the soleus muscle of the decerebrate cat during stretching of the muscle under controlled conditions.2. Dimethothiazine in doses of 1 to 4 mg/kg intravenously reduced the disc...

journal_title：British journal of pharmacology

authors： Maxwell DR,Rhodes KF

更新日期：1970-07-01 00:00:00

abstract：:1 The effects of purported prostaglandin synthesis inhibitors on steroid and prostaglandin (E and F) release from trypsin-dispersed cat adrenocortical cells were investigated. 2 Low indomethacin concentrations potentiated adrenocorticotrophin (ACTH)-evoked prostaglandin and steroid release, whereas higher concentratio...

journal_title：British journal of pharmacology

authors： Laychock SG,Rubin RP

更新日期：1976-06-01 00:00:00