The site of general anaesthesia and cytochrome P450 oxygenases: similarities defined by straight chain and cyclic alcohols.

abstract：BACKGROUND AND PURPOSE:While remifentanil can be used either during labour or fetal surgery, more should be known about the transplacental transfer of this opioid. The aim of this study was to investigate the placental transfer and haemodynamic effects of remifentanil after i.v. administration to pregnant ewes. EXPERI...

journal_title：British journal of pharmacology

authors： Coonen JB,Marcus MA,Joosten EA,van Kleef M,Neef C,van Aken H,Gogarten W

更新日期：2010-12-01 00:00:00

abstract：:1. The effect of intradermally injected endotoxin on skin blood flow was investigated in anaesthetized male Wistar rats in vivo. 2. Local skin blood flow changes were measured hourly for 6 h in the shaved dorsal skin with a laser-Doppler flow probe and compared to changes in control sites which had been injected with ...

journal_title：British journal of pharmacology

authors： Warren JB,Coughlan ML,Williams TJ

更新日期：1992-08-01 00:00:00

abstract：:1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency...

journal_title：British journal of pharmacology

authors： Newbould BB

更新日期：1969-03-01 00:00:00

abstract：:1 This study investigated the effects of soluble complement receptor type 1 (sCR1) or sCR1sLex, agents which function as a complement inhibitor or as a combined complement inhibitor and selectin adhesion molecule antagonist, respectively, on the infarct size and cardiac troponin T (cTnT) release caused by regional myo...

journal_title：British journal of pharmacology

authors： Zacharowski K,Otto M,Hafner G,Marsh HC Jr,Thiemermann C

更新日期：1999-11-01 00:00:00

abstract：:Three genes encode the small-conductance Ca(2+)-activated K(+) channels (SK channels). We have stably expressed hSK1 and rSK2 in HEK 293 cells and addressed the pharmacology of these subtypes using whole-cell patch clamp recordings. The bee venom peptide apamin blocked hSK1 as well as rSK2 with IC(50) values of 3.3 nM...

journal_title：British journal of pharmacology

authors： Strøbaek D,Jørgensen TD,Christophersen P,Ahring PK,Olesen SP

更新日期：2000-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Acute activation of κ opioid (KOP) receptors results in anticocaine-like effects, but adverse effects, such as dysphoria, aversion, sedation and depression, limit their clinical development. Salvinorin A, isolated from the plant Salvia divinorum, and its semi-synthetic analogues have been shown t...

journal_title：British journal of pharmacology

authors： Simonson B,Morani AS,Ewald AW,Walker L,Kumar N,Simpson D,Miller JH,Prisinzano TE,Kivell BM

更新日期：2015-01-01 00:00:00

abstract：:1 Morphine-theophylline interactions were investigated in both acute and narcotic-dependent preparations, in vitro and in vivo, using four different experimental models: LD50 doses of morphine and naloxone in the mouse; naloxone-induced contractions in the electrically-stimulated and opiate-dependent isolated ileum of...

journal_title：British journal of pharmacology

authors： Brailowsky S,Guerrero-Muñoz F,Luján M,Shkurovich M

更新日期：1981-08-01 00:00:00

abstract：:1. This study describes the effects of hypoxia on relaxing responses and cAMP production induced by the known vasodilator peptides: alphaCGRP, amylin (AMY) and adrenomedullin (AM) on isolated pig coronary arteries in vitro. 2. Hypoxic incubation increased the vasorelaxant effect of alphaCGRP (four-fold; P<0.05), AMY (...

journal_title：British journal of pharmacology

authors： Hasbak P,Eskesen K,Schifter S,Edvinsson L

更新日期：2005-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Asthenozoospermia is a leading cause of male infertility, but development of pharmacological agents to improve sperm motility is hindered by the lack of effective screening platforms and knowledge of suitable molecular targets. We have demonstrated that a high-throughput screening (HTS) strategy ...

journal_title：British journal of pharmacology

authors： McBrinn RC,Fraser J,Hope AG,Gray DW,Barratt CLR,Martins da Silva SJ,Brown SG

更新日期：2019-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Translation of non-clinical markers of delayed ventricular repolarization to clinical prolongation of the QT interval corrected for heart rate (QTc) (a biomarker for torsades de pointes proarrhythmia) remains an issue in drug discovery and regulatory evaluations. We retrospectively analysed 150 d...

journal_title：British journal of pharmacology

authors： Park E,Gintant GA,Bi D,Kozeli D,Pettit SD,Pierson JB,Skinner M,Willard J,Wisialowski T,Koerner J,Valentin JP

更新日期：2018-02-01 00:00:00

abstract：:1. The effects of intradermally injected prostaglandins (PGs) E(1), E(2), F(1alpha) and F(2alpha) have been examined in the rat and in man.2. PGE(1) and PGE(2) caused an increase in local vascular permeability in rat skin; their potency was comparable with that of other putative mediators of inflammation (histamine, b...

journal_title：British journal of pharmacology

authors： Crunkhorn P,Willis AL

更新日期：1971-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GPR18 is a recently deorphaned lipid receptor that is activated by the endogenous lipid N-arachidonoyl glycine (NAGly) as well the behaviourally inactive atypical cannabinoid, abnormal cannabidiol (Abn-CBD). The presence and/or function of any GPR18-based ocular signalling system remain essential...

journal_title：British journal of pharmacology

authors： Caldwell MD,Hu SS,Viswanathan S,Bradshaw H,Kelly ME,Straiker A

更新日期：2013-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Non-alcoholic fatty liver disease (NAFLD) is considered to be one of the most common chronic liver diseases across worldwide. Astaxanthin (Ax) is a carotenoid, and beneficial effects of astaxanthin, including anti-oxidative, anti-inflammatory, and anti-tumour activity, have been identified. The p...

journal_title：British journal of pharmacology

authors： Wu L,Mo W,Feng J,Li J,Yu Q,Li S,Zhang J,Chen K,Ji J,Dai W,Wu J,Xu X,Mao Y,Guo C

更新日期：2020-08-01 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. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-...

journal_title：British journal of pharmacology

authors： Snowdy S,Liang HX,Blackburn B,Lum R,Nelson M,Wang L,Pfister J,Sharma BP,Wolff A,Belardinelli L

更新日期：1999-01-01 00:00:00

abstract：:1. The potencies of some beta-adrenoreceptor blocking drugs in reducing noradrenaline uptake by the isolated heart were compared with their potencies in reducing the release of noradrenaline from the heart by tyramine.2. Of the drugs tested, propranolol, pronethalol and dichloroisoprenaline were the most potent in blo...

journal_title：British journal of pharmacology

authors： Foo JW,Jowett A,Stafford A

更新日期：1968-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The thiourea derivative KB-R7943, originally developed as inhibitor of the plasma membrane Na(+)/Ca(2+) exchanger, has been shown to protect against myocardial ischemia-reperfusion injury. We have studied here its effects on mitochondrial Ca(2+) fluxes. EXPERIMENTAL APPROACH:[Ca(2+)] in cytosol,...

journal_title：British journal of pharmacology

authors： Santo-Domingo J,Vay L,Hernández-Sanmiguel E,Lobatón CD,Moreno A,Montero M,Alvarez J

更新日期：2007-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Azithromycin has been reported to modify activation of macrophages towards the M2 phenotype. Here, we have sought to identify the mechanisms underlying this modulatory effect of azithromycin on human monocytes, classically activated in vitro. EXPERIMENTAL APPROACH:Human blood monocytes were prim...

journal_title：British journal of pharmacology

authors： Vrančić M,Banjanac M,Nujić K,Bosnar M,Murati T,Munić V,Stupin Polančec D,Belamarić D,Parnham MJ,Eraković Haber V

更新日期：2012-03-01 00:00:00

abstract：:1. The sinus node inhibitors UL FS 49 and DK-AH 269 reduce heart rate by slowing diastolic depolarization rate in the sino-atrial (SA) node, which might originate from the use-dependent blockade of a hyperpolarization-activated current If. A hyperpolarization-activated current Ih, which is present in many types of neu...

journal_title：British journal of pharmacology

authors： Raes A,Van de Vijver G,Goethals M,van Bogaert PP

更新日期：1998-10-01 00:00:00

abstract：:1. The ability of the putative, selective post-junctional alpha 2-adrenoceptor antagonist, SK&F 104078 to antagonize the effects of structurally-diverse agonists at pre-junctional alpha 2-adrenoceptors in the guinea-pig ileum and rat vas deferens in vitro and in the rat heart in vivo, and at post-junctional alpha 2-ad...

journal_title：British journal of pharmacology

authors： Akers I,Coates J,Drew GM,Sullivan AT

更新日期：1991-04-01 00:00:00

abstract：:The aim of the present study was to determine whether inhibition of cyclic nucleotide phosphodiesterase (PDE) modulates the stimulated generation of the cytokines, interleukin-4 (IL-4) and IL-13, from human basophils. This was addressed by evaluating the effects of both nonselective and selective inhibitors of PDEs on...

journal_title：British journal of pharmacology

authors： Eskandari N,Wickramasinghe T,Peachell PT

更新日期：2004-08-01 00:00:00

abstract：:1 Anthopleurin-B (AP-B, greater than 3 x 10(-9) M), a newly isolated polypeptide from sea anemone (Anthopleura xanthogrammica), caused powerful rhythmic contractions in the guinea-pig isolated vas deferens. The other polypeptides anthopleurin-A from A. xanthogrammica and anthopleurin-C from A. elegantissima, elicited ...

journal_title：British journal of pharmacology

authors： Norton TR,Ohizumi Y,Shibata S

更新日期：1981-09-01 00:00:00

abstract：:1. Inhibition of mechanical activity in longitudinal muscle strips of rabbit duodenum was induced by perivascular and intramural nerve stimulation.2. The effects of perivascular stimulation were abolished by phentolamine + propranolol, guanethidine, reserpine and by tetrodotoxin. The effects of intramural stimulation ...

journal_title：British journal of pharmacology

authors： Weston AH

更新日期：1973-06-01 00:00:00

abstract：:1. Both in mammalian tissues and in transfected cells, only low levels of alpha1D-adrenoceptors are detected in radioligand binding studies. It has been implicated that the comparatively long N-terminal tail of the alpha1D-adrenoceptor is responsible for the inefficient surface expression of the receptor. 2. In the pr...

journal_title：British journal of pharmacology

authors： Petrovska R,Kapa I,Klovins J,Schiöth HB,Uhlén S

更新日期：2005-03-01 00:00:00

abstract：:1. It has previously been shown that the antimigraine drug, sumatriptan, a putative 5-HT1D receptor agonist, decreases porcine common carotid and arteriovenous anastomotic blood flows, but slightly increases the arteriolar (capillary) blood flow to the skin and ears. Interestingly, such responses, being mediated by 5-...

journal_title：British journal of pharmacology

authors： De Vries P,Heiligers JP,Villalón CM,Saxena PR

更新日期：1996-05-01 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 actions of parathyroid hormone (PTH) are antagonized in vitro by the peptide [Nle-8, Nle-18, Tyr-34]-bPTH-(3-34)amide, an analogue of PTH. In this paper, the actions of the inhibitory peptide were investigated in vivo. 2 Native parathyroid hormone (bPTH-(1-84)), administered i.v. (0.17-1.51 nmol in volume of 0.3...

journal_title：British journal of pharmacology

authors： Gray DA,Parsons JA,Potts JT Jr,Rosenblatt M,Stevenson RW

更新日期：1982-06-01 00:00:00

abstract：:The POZ domain Krüppel-like zinc finger transcription repressor (POK family) contains many important molecules, including RP58, Bcl6 and PLZF. They function as transcription repressors via chromatin remodelling and histone deacetylation and are known to be involved in the development and tumourigenesis of various orga...

journal_title：British journal of pharmacology

authors： Okado H

更新日期：2020-09-22 00:00:00

abstract：:In the present study we used a bioassay to study the effects of peroxynitrite (ONOO-) on angiotensin II (A-II)-triggered tension in isolated bovine coronary arteries in order to show the consequences of the previously reported PGI2-synthase inhibition by ONOO- in this model. The following results were obtained: 1. 1 m...

journal_title：British journal of pharmacology

authors： Zou M,Jendral M,Ullrich V

更新日期：1999-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) plays a role in thermogenesis. The exogenous compound capsaicin increased SERCA-mediated ATP hydrolysis not coupled to Ca²⁺ transport. Here, we have sought to identify endogenous compounds that may function as SERCA uncoupling agents. EXPERIMENTAL A...

journal_title：British journal of pharmacology

authors： Mahmmoud YA,Gaster M

更新日期：2012-08-01 00:00:00