The effects of methyl beta-carboline-3-carboxylate on social interaction and locomotor activity when microinjected into the nucleus raphé dorsalis of the rat.

abstract：:1 Hypolipidaemic agents may increase biliary cholesterol in man, inducing a supersaturated bile. 2 To evaluate this possible side-effect, we have studied bile lipid secretion over a period of 8 h with intact enterohepatic circulation and 4 h with complete interruption in rats treated for two months with a salt of chol...

journal_title：British journal of pharmacology

authors： Aldini R,Barbara L,Benelli A,Borzatta V,Geminiani S,Mascellani G,Morselli A,Roda A,Roda E

更新日期：1981-11-01 00:00:00

abstract：:The binding of a series of amide derivatives of methotrexate to Lactobacillus casei dihydrofolate reductase has been studied by inhibition constant measurements and by 1H n.m.r. spectroscopy. Amide modification of the alpha-carboxylate of methotrexate was found to prevent interaction of the gamma-carboxylate with the ...

journal_title：British journal of pharmacology

authors： Antonjuk DJ,Birdsall B,Cheung HT,Clore GM,Feeney J,Gronenborn A,Roberts GC,Tran TQ

更新日期：1984-02-01 00:00:00

abstract：:1. The effect of clofibrate (CFB), bezafibrate (BFB), and gemfibrozil (GFB) on plasma lipoprotein (VLDL and LDL) concentration, composition and resistance to copper-induced oxidation has been studied in male Sprague-Dawley rats after a 15 day treatment. 2. Plasma triglyceride levels were reduced by CFB (41%) and BFB (...

journal_title：British journal of pharmacology

authors： Vázquez M,Merlos M,Adzet T,Laguna JC

更新日期：1996-03-01 00:00:00

abstract：:Extensive in vitro and in vivo studies have shown that cannabinoid drugs have neuroprotective properties and suggested that the endocannabinoid system may be involved in endogenous neuroprotective mechanisms. On the other hand, neurotoxic effects of cannabinoids in vitro and in vivo were also described. Several possib...

journal_title：British journal of pharmacology

authors： Sarne Y,Asaf F,Fishbein M,Gafni M,Keren O

更新日期：2011-08-01 00:00:00

abstract：:1. This study was undertaken to determine the effects of OSW-1 (3 beta, 16 beta, 17 alpha-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)- (1-->3)-(2-O-acetyl-alpha-L-arabinopyranoside)) on the pituitary-ovarian system and the functions of aortic smooth muscle. 2. A single s.c. injection...

journal_title：British journal of pharmacology

authors： Tamura K,Honda H,Mimaki Y,Sashida Y,Kogo H

更新日期：1997-08-01 00:00:00

abstract：:1. Phenylarsine oxide (PAO) is commonly used to inhibit tyrosine phosphatase activity. However, PAO can affect a variety of different processes because of its ability to promote sulfhydryl oxidation. In the present study, we investigated the effects that PAO has on basal and beta-adrenergically stimulated L-type Ca(2+...

journal_title：British journal of pharmacology

authors： Sims C,Harvey RD

更新日期：2004-06-01 00:00:00

abstract：:1. Prostaglandins and the vasodilator neuropeptide, calcitonin-gene related peptide (CGRP), have both been implicated in the pathogenesis of migraine headache. We have used primary cultures of adult rat trigeminal neurones to examine the effects of prostanoids on CGRP release in vitro. 2. CGRP release was stimulated b...

journal_title：British journal of pharmacology

authors： Jenkins DW,Feniuk W,Humphrey PP

更新日期：2001-11-01 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：:1. Morphine, oxotremorine and physostigmine showed antinociceptive activity in mice using the hot plate reaction time test.2. The action of morphine, but not that of oxotremorine, was antagonized by naloxone and by nalorphine, whereas the effect of physostigmine was unaffected by naloxone and increased by nalorphine.3...

journal_title：British journal of pharmacology

authors： Pleuvry BJ,Tobias MA

更新日期：1971-12-01 00:00:00

abstract：:The administration of arachidonic acid (AA) to the isolated perfused heart of the rat usually produced biphasic coronary responses characterized by initial vasoconstriction followed by prolonged vasodilatation. However, some responses were predominantly vasoconstrictor or vasodilator. The non-steroidal anti-inflammato...

journal_title：British journal of pharmacology

authors： Belo SE,Talesnik J

更新日期：1982-02-01 00:00:00

abstract：:In electrophysiological measurements the beta-carboline ethyl 6-benzyloxy-beta-carboline-3-carboxylate (ZK 91085) acts as a positive allosteric modulator on rat recombinant alpha1beta2gamma2 GABA(A) receptors and binds with high affinity (IC50-1.5 nM) to the [3H]-flunitrazepam site. Flumazenil was able to partially co...

journal_title：British journal of pharmacology

authors： Thomet U,Baur R,Scholze P,Sieghart W,Sigel E

更新日期：1999-07-01 00:00:00

abstract：:The effects of intravenous sufentanil and pre-administration of N-methyl-D-aspartate (NMDA) receptor antagonists were tested on a reflex triggered by C-fibre activation. The reflex was elicited by electrical stimulation of the sural nerve and recorded from the ipsilateral biceps femoris muscle in halothane anaesthetiz...

journal_title：British journal of pharmacology

authors： Adam F,Gairard AC,Chauvin M,Le Bars D,Guirimand F

更新日期：2001-08-01 00:00:00

abstract：:1. The accumulation of (3)H-gamma-aminobutyric acid (GABA) by the isolated rat retina has been measured.2. When retinae were incubated at 37 degrees C in a medium containing (3)H-GABA, tissue:medium ratios of about 25:1 were attained after a 30 min incubation.3. After incubations of 40 min at 37 degrees C, almost all ...

journal_title：British journal of pharmacology

authors： Goodchild M,Neal MJ

更新日期：1973-03-01 00:00:00

abstract：:1. In the presence of indomethacin (IM, 10 microM) and N omega-nitro-L- arginine (L-NOARG, 0.3 mM), acetylcholine (ACh) induces an endothelium-dependent smooth muscle hyperpolarization and relaxation in the rat isolated hepatic artery. The potassium (K) channel inhibitors, tetrabutylammonium (TBA, 1 mM) and to a lesse...

journal_title：British journal of pharmacology

authors： Zygmunt PM,Högestätt ED

更新日期：1996-04-01 00:00:00

abstract：:1. The effects of the metabotropic glutamate receptor (mGluR) antagonist, L-2-amino-3-phosphonopropionate (L-AP3) on phosphoinositide turnover in neonatal rat cerebral cortex slices has been investigated. 2. At concentrations of < or = 300 microM, L-AP3 inhibited total [3H]-inositol phosphate ([3H]-InsPx) and Ins(1,4,...

journal_title：British journal of pharmacology

authors： Mistry R,Prabhu G,Godwin M,Challiss RA

更新日期：1996-03-01 00:00:00

abstract：:Antidromic stimulation of sensory peripheral branches of the trigeminal system (mental nerve) leads to cutaneous vasodilatation and increases vascular permeability in the rat. Antidromic vasodilatation is observed only at high intensity stimulation (10 V, 15 Hz, 0.2 or 5 ms) supporting the participation of afferent C-...

journal_title：British journal of pharmacology

authors： Couture R,Cuello AC,Henry JL

更新日期：1985-03-01 00:00:00

abstract：:Rodent models of chronic pain may elucidate pathophysiological mechanisms and identify potential drug targets, but whether they predict clinical efficacy of novel compounds is controversial. Several potential analgesics have failed in clinical trials, in spite of strong animal modelling support for efficacy, but there...

journal_title：British journal of pharmacology

authors： Berge OG

更新日期：2011-10-01 00:00:00

abstract：:1. Voltage-operated calcium channel (VOCC) antagonists are effective antihypertensive and antianginal agents but they also depress myocardial contractility. 2. We compared four L-type calcium channel antagonists, felodipine, nifedipine, amlodipine and verapamil and a relatively T-type selective calcium channel antagon...

journal_title：British journal of pharmacology

authors： Sarsero D,Fujiwara T,Molenaar P,Angus JA

更新日期：1998-09-01 00:00:00

abstract：:1. The effect of histamine H1-receptor stimulation on inositol phospholipid hydrolysis has been investigated in the hamster vas deferens smooth muscle cell line, DDT1MF-2. 2. Histamine (EC50 = 27 microM) stimulated the accumulation of [3H]-inositol phosphates in DDT1MF-2 cells prelabelled with [3H]-myo-inositol. 2-Thi...

journal_title：British journal of pharmacology

authors： White TE,Dickenson JM,Hill SJ

更新日期：1993-01-01 00:00:00

abstract：:1. Several cations (Ba2+, Cd2+, Co2+, Cu2+, Mn2+, Ni2+, Zn2+ and La3+, all as chloride salts, 1-1000 microM) were tested in the guinea-pig urinary bladder for their ability to: (i) modify contractile responses to electrical field stimulation (EFS), ATP, alpha,beta-methylene ATP (alpha,beta-meATP), carbachol (CCh), and...

journal_title：British journal of pharmacology

authors： Ziganshin AU,Ziganshina LE,Hoyle CH,Burnstock G

更新日期：1995-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Screening of 12,000 compounds for binding affinity to the synaptic vesicle protein 2A (SV2A), identified a high-affinity pyrrolidone derivative, brivaracetam (ucb 34714). This study examined its pharmacological profile in various in vitro and in vivo models of seizures and epilepsy, to evaluate i...

journal_title：British journal of pharmacology

authors： Matagne A,Margineanu DG,Kenda B,Michel P,Klitgaard H

更新日期：2008-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Transient receptor potential melastatin 3 (TRPM3) proteins form non-selective but calcium-permeable membrane channels, rapidly activated by extracellular application of the steroid pregnenolone sulphate and the dihydropyridine nifedipine. Our aim was to characterize the steroid binding site by an...

journal_title：British journal of pharmacology

authors： Drews A,Mohr F,Rizun O,Wagner TF,Dembla S,Rudolph S,Lambert S,Konrad M,Philipp SE,Behrendt M,Marchais-Oberwinkler S,Covey DF,Oberwinkler J

更新日期：2014-02-01 00:00:00

abstract：:The aims of this study were to develop a technique to measure blood flow in the mouse ear and to investigate the nature of the vasodilator mediator(s) involved in the response to capsaicin. The response to capsaicin, applied topically, was investigated in anaesthetized CD1 or Sv129+C57BL/6 wild-type (+/+) or NK(1) rec...

journal_title：British journal of pharmacology

authors： Grant AD,Gerard NP,Brain SD

更新日期：2002-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhalation of the superantigen,staphylococcal enterotoxin B (SEB), leads to the activation of the host T and invariant natural killer (iNK) T cells, thereby resulting in acute lung inflammation and respiratory failure but the underlying mechanism(s) of disease remain elusive, with limited treatme...

journal_title：British journal of pharmacology

authors： Rieder SA,Nagarkatti P,Nagarkatti M

更新日期：2012-11-01 00:00:00

abstract：:Histamine has been one of the most studied substances in medicine, playing a major role in diverse (patho)physiological processes. It elicits its multifaceted modulatory functions by activating four types of GPCRs, designated as H1-4 . Despite the heterogeneity and the complexity of histamine receptor pharmacology, ma...

journal_title：British journal of pharmacology

authors： Tiligada E,Ennis M

更新日期：2020-02-01 00:00:00

abstract：:1 Poly (ADP-ribose) synthetase (PARS) is a nuclear enzyme activated by strand breaks in DNA, which are caused by reactive oxygen species (ROS). Here we investigate the effects of the PARS inhibitors 3-aminobenzamide (3-AB), nicotinamide and 1,5-dihydroxyisoquinoline (ISO) on the circulatory failure and the organ injur...

journal_title：British journal of pharmacology

authors： McDonald MC,Filipe HM,Thiemermann C

更新日期：1999-11-01 00:00:00

abstract：:The profiles of four analogues of idazoxan have been examined at alpha-adrenoceptors and the results compared to those obtained with idazoxan and yohimbine. The compounds possessed either a methyl (RX 801079), ethyl (RX 811033), n-propyl (RX 811054) or isopropenyl (RX 811005) group at the two position of idazoxan. The...

journal_title：British journal of pharmacology

authors： Doxey JC,Roach AG,Strachan DA,Virdee NK

更新日期：1984-11-01 00:00:00

abstract：UNLABELLED:Midkine (MK) is a heparin-binding growth factor or cytokine and forms a small protein family, the other member of which is pleiotrophin. MK enhances survival, migration, cytokine expression, differentiation and other activities of target cells. MK is involved in various physiological processes, such as devel...

journal_title：British journal of pharmacology

authors： Muramatsu T

更新日期：2014-02-01 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：:Endothelin-1 (ET-1) is a peptide hormone produced within the myocardium which may modulate myocardial contractility in a paracrine-autocrine fashion. In the majority of species, ET-1 has a direct positive inotropic effect on the myocardium that involves both increased myofilament Ca(2+) sensitivity and increased Ca(2+...

journal_title：British journal of pharmacology

authors： James AF

更新日期：2007-10-01 00:00:00