Effect of frusemide, ethacrynic acid and indanyloxyacetic acid on spontaneous Ca-activated currents in rabbit portal vein smooth muscle cells.

abstract：:1 Contractions of the cat nictitating membrane were elicited on stimulation of the internal carotid nerve, and the effects were studied of desipramine and two inhibitors of catechol-O-methyltransferase, U-0521 and pyrogallol, on the subsequent relaxation of the muscle. 2 The relaxation of the nictitating membrane occu...

journal_title：British journal of pharmacology

authors： Eccles R,Maclean AG

更新日期：1978-04-01 00:00:00

abstract：:1. This study was undertaken to investigate whether, after a brief exposure of guinea-pig isolated ileum and rabbit jejunum to bremazocine, a kappa-opioid agonist also possessing antagonist activity at mu-opioid receptors, the addition of opioid antagonists produced withdrawal contractures. Our aim was to verify in th...

journal_title：British journal of pharmacology

authors： Valeri P,Morrone LA,Romanelli L,Amico MC

更新日期：1995-03-01 00:00:00

abstract：:1. Regulation of the increase in inositol-1,4,5-trisphosphate (IP3) production and intracellular Ca2+ concentration ([Ca2+]i by protein kinase C (PKC) was investigated in canine cultured tracheal smooth muscle cells (TSMCs). Stimulation of TSMCs by 5-hydroxytryptamine (5-HT) caused an initial transient [Ca2+]i peak fo...

journal_title：British journal of pharmacology

authors： Yang CM,Fen LW,Tsao HL,Chiu CT

更新日期：1997-07-01 00:00:00

abstract：:1. Anaesthetized, open-chest dogs were subjected to 60 min of left circumflex coronary artery occlusion followed by 90 min of reperfusion. Endothelium-dependent and -independent relaxant responses of the isolated coronary arterial rings were then investigated. 2. The endothelium-dependent, acetylcholine-induced relaxa...

journal_title：British journal of pharmacology

authors： Sobey CG,Dalipram RA,Dusting GJ,Woodman OL

更新日期：1992-03-01 00:00:00

abstract：:1. The effects of tacrine (9-amino-1,2,3,4-tetrahydroacridine), velnacrine (HP029, 9-amino-1,2,3,4-tetrahydroacridin-1-ol maleate), suronacrine (HP128, 9-benzylamino-1,2,3,4-tetrahydroacridin-1-ol maleate), and 3,4-diaminopyridine on neuromuscular transmission were compared on isolated nerve-muscle preparations. 2. Ta...

journal_title：British journal of pharmacology

authors： Braga MF,Harvey AL,Rowan EG

更新日期：1991-04-01 00:00:00

abstract：:1. We have evaluated the selectivity of ketoprofen and two novel nonsteroidal anti-inflammatory drugs, N-[2-(cyclohexyloxy)-4-nitrophenyl]methanesulphonamide (NS-398) and 5-methanesulphonamido-6-(2,4-difluorothiophenyl)-1-indano ne (L-745,337), in inhibiting the cyclo-oxygenase activity of prostaglandin endoperoxide s...

journal_title：British journal of pharmacology

authors： Panara MR,Greco A,Santini G,Sciulli MG,Rotondo MT,Padovano R,di Giamberardino M,Cipollone F,Cuccurullo F,Patrono C

更新日期：1995-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cholecystokinin (CCK) is secreted by intestinal I cells and regulates important metabolic functions. In pancreatic islets, CCK controls beta cell functions primarily through CCK1 receptors, but the signalling pathways downstream of these receptors in pancreatic beta cells are not well defined. E...

journal_title：British journal of pharmacology

authors： Ning SL,Zheng WS,Su J,Liang N,Li H,Zhang DL,Liu CH,Dong JH,Zhang ZK,Cui M,Hu QX,Chen CC,Liu CH,Wang C,Pang Q,Chen YX,Yu X,Sun JP

更新日期：2015-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Alterations in the tyrosine kinase enzyme RET are found in thyroid and lung cancer. While RET TK inhibitors (TKIs) are used to treat thyroid cancer and are in clinical trials for RET fusion-positive non-small cell lung cancer, the impact of mutations in the RET kinase domain on drug sensitivity i...

journal_title：British journal of pharmacology

authors： Liu X,Shen T,Mooers BHM,Hilberg F,Wu J

更新日期：2018-09-01 00:00:00

abstract：:The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more deta...

journal_title：British journal of pharmacology

authors： Alexander SP,Christopoulos A,Davenport AP,Kelly E,Marrion NV,Peters JA,Faccenda E,Harding SD,Pawson AJ,Sharman JL,Southan C,Davies JA,CGTP Collaborators.

更新日期：2017-12-01 00:00:00

abstract：:Recent clinical studies have demonstrated that angiotensin II type 1 (AT(1) ) receptor blockers (ARBs) reduce the onset of stroke, stroke severity and the incidence and progression of Alzheimer's disease and dementia. We can expect that ARBs exert these effects by both AT(1) receptor blockade and angiotensin II type 2...

journal_title：British journal of pharmacology

authors： Horiuchi M,Mogi M

更新日期：2011-07-01 00:00:00

abstract：:1. The role of nitic oxide (NO) derived from L-arginine in the regional vasodilator effects of endothelin-1 has been investigated in anaesthetized, spontaneously hypertensive (SH) rats in which autonomic reflexes were abolished by ganglion blockade. The experimental design incorporated animals infused with phenylephri...

journal_title：British journal of pharmacology

authors： Fozard JR,Part ML

更新日期：1992-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The regulation of vascular soluble guanylyl cyclase (sGC) expression by nitric oxide (NO) is still under discussion. In vitro, NO has been shown to downregulate the expression of sGC but it is unclear if this mechanism is operative in vivo and occurs during nitrate treatment. EXPERIMENTAL APPROA...

journal_title：British journal of pharmacology

authors： Oppermann M,Dao VT,Suvorava T,Bas M,Kojda G

更新日期：2008-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In small arteries, small conductance Ca²⁺-activated K⁺ channels (SK(Ca)) and intermediate conductance Ca²⁺-activated K⁺ channels (IK(Ca)) restricted to the vascular endothelium generate hyperpolarization that underpins the NO- and PGI₂-independent, endothelium-derived hyperpolarizing factor respo...

journal_title：British journal of pharmacology

authors： Yarova PL,Smirnov SV,Dora KA,Garland CJ

更新日期：2013-06-01 00:00:00

abstract：:1 Tissue was taken from guinea-pigs that had been injected with guanethidine (100 mg/kg, i.p.) 24 h before they were killed, and from paired control animals.2 Pretreatment with guanethidine caused a significant, substantial, and sometimes complete reduction of the nerve-mediated contractions of the vas deferens. There...

journal_title：British journal of pharmacology

authors： Furness JB

更新日期：1974-01-01 00:00:00

abstract：:1 The possible involvement of N-methyl-D-aspartate (NMDA)-receptors in epileptiform synaptic activity in the kainic acid (KA) lesioned hippocampus was investigated. In this chronic model of epilepsy there is a loss of both the early and the late components of synaptic inhibition as well as changes in the membrane prop...

journal_title：British journal of pharmacology

authors： Ashwood TJ,Wheal HV

更新日期：1987-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Benzofurans are newly used psychoactive substances, but their pharmacology is unknown. The aim of the present study was to pharmacologically characterize benzofurans in vitro. EXPERIMENTAL APPROACH:We assessed the effects of the benzofurans 5-APB, 5-APDB, 6-APB, 6-APDB, 4-APB, 7-APB, 5-EAPB and ...

journal_title：British journal of pharmacology

authors： Rickli A,Kopf S,Hoener MC,Liechti ME

更新日期：2015-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Retinoids, through their activation of retinoic acid receptors (RARs) and retinoid X receptors, regulate diverse cellular processes, and pharmacological intervention in their actions has been successful in the treatment of skin disorders and cancers. Despite the many beneficial effects, administr...

journal_title：British journal of pharmacology

authors： Yin S,Luo J,Qian A,Yu W,Hu H

更新日期：2014-03-01 00:00:00

abstract：:1. The vasodilator effects of arginine, nitric oxide (NO), acetylcholine (ACh) and sodium nitroprusside (NP) in the noradrenaline-preconstricted ('high tone') perfused rat kidney have been examined. 2. L-Arginine (0.6-23 mumol) caused a biphasic change in renal perfusion pressure. D-Arginine (0.6-23 mumol) was without...

journal_title：British journal of pharmacology

authors： Bhardwaj R,Moore PK

更新日期：1989-07-01 00:00:00

abstract：:1. The relationships between the density of dopamine D4.4 receptors and the agonist efficacies of L-745,870 (3-(4-[4-chlorophhenyl]piperazin-1-yl)-methyl-1H-pyrrolo [2, 3-b]pyridine) and U-101958 ((1-benzyl-piperidin-4-yl)-(3-isopropoxy-pyridin-2-yl)-methyl-a min e) were investigated in Chinese hamster ovary (CHO) cel...

journal_title：British journal of pharmacology

authors： Gazi L,Bobirnac I,Danzeisen M,Schüpbach E,Langenegger D,Sommer B,Hoyer D,Tricklebank M,Schoeffter P

更新日期：1999-10-01 00:00:00

abstract：:The effect of adenosine on transepithelial ion transport was investigated in isolated preparations of murine trachea mounted in Ussing chambers. The possible regulation of adenosine receptors in an established model of allergic airway inflammation was also investigated. Mucosally applied adenosine caused increases in ...

journal_title：British journal of pharmacology

authors： Kornerup KN,Page CP,Moffatt JD

更新日期：2005-04-01 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：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 The effect of compound 48/80 was studied on the twitch-like contractions of the longitudinal muscle of guinea-pig ileum induced by electrical stimulation of intramural cholinergic nerves. 2 Compound 48/80 alone, at concentrations up to 30 microgram/ml, had no effect on the twitch contractions. The contraction to exo...

journal_title：British journal of pharmacology

authors： Kamikawa Y,Shimo Y

更新日期：1978-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Biased GPCR ligands are able to engage with their target receptor in a manner that preferentially activates distinct downstream signalling and offers potential for next generation therapeutics. However, accurate quantification of ligand bias in vitro is complex, and current best practice is not a...

journal_title：British journal of pharmacology

authors： Winpenny D,Clark M,Cawkill D

更新日期：2016-04-01 00:00:00

abstract：:In recent years, late-stage clinical drug development that primarily focuses on urogenital targets has centered around four areas of medical need (both unmet need and aiming to improve on existing therapies). These include male sexual dysfunction (MSD), female sexual dysfunction (FSD), prostatic pathology (neoplastic,...

journal_title：British journal of pharmacology

authors： Azam U

更新日期：2006-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Emesis is a multi-system reflex, which is usually investigated using in vivo models. The aim of the study is to compare the response induced by emetic compounds across species and investigate whether dogs, ferrets and rats are all similarly predictive of humans. EXPERIMENTAL APPROACH:A systemati...

journal_title：British journal of pharmacology

authors： du Sert NP,Holmes AM,Wallis R,Andrews PL

更新日期：2012-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-alcoholic hepatic fatty liver disease (NAFLD) is a manifestation of the metabolic syndrome in the liver and non-alcoholic steatohepatitis (NASH) represents its advanced stage. R17 derived from bouchardatine, shows benefits in the metabolic syndrome, but has not been tested in the liver. The p...

journal_title：British journal of pharmacology

authors： Rao Y,Lu YT,Li C,Song QQ,Xu YH,Xu Z,Hu YT,Yu H,Gao L,Gu LQ,Ye JM,Huang ZS

更新日期：2019-08-01 00:00:00

abstract：:delta 9-Tetrahydrocannabinol (delta 9-THC) was injected into the preoptic area of the anterior hypothalamus or into the third or fourth cerebral ventricle of the conscious mouse through a chronically implanted cannula and the effects on body temperature and oxygen consumption rate were measured. At an ambient temperat...

journal_title：British journal of pharmacology

authors： Fitton AG,Pertwee RG

更新日期：1982-02-01 00:00:00

abstract：:Cyclic nucleotide phosphodiesterases (PDEs) that specifically inactivate the intracellular messengers cAMP and cGMP in a compartmentalized manner represent an important enzyme class constituted by 11 gene-related families of isozymes (PDE1 to PDE11). Downstream receptors, PDEs play a major role in controlling the sign...

journal_title：British journal of pharmacology

authors： Keravis T,Lugnier C

更新日期：2012-03-01 00:00:00

abstract：:1. The possible roles of endothelial and smooth muscle cell hyperpolarization and nitric oxide (NO) in endothelium-dependent relaxation were examined in isolated rings of pig right coronary artery. 2. The effects of hyperpolarization were prevented with high K+ (30-125 mM), isotonic Krebs solutions. Functional antagon...

journal_title：British journal of pharmacology

authors： Kilpatrick EV,Cocks TM

更新日期：1994-06-01 00:00:00