WAY-100635 AND GR127935 - EFFECTS ON 5-HYDROXYTRYPTAMINE-CONTAINING NEURONS

被引：46

作者：

CRAVEN, R

GRAHAMESMITH, D

NEWBERRY, N

机构：

[1] UNIV OXFORD,RADCLIFFE INFIRM,SMITHKLINE BEECHAM CTR APPL NEUROPSYCHOBIOL,OXFORD OX2 6HE,ENGLAND

[2] UNIV OXFORD,RADCLIFFE INFIRM,DEPT CLIN PHARMACOL,OXFORD OX2 6HE,ENGLAND

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1994年 / 271卷 / 01期

基金：

英国惠康基金;

关键词：

DORSAL RAPHE; 5-HT; (5-HYDROXYTRYPTAMINE; SEROTONIN); (GUINEA-PIG);

D O I：

10.1016/0014-2999(94)90289-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride (WAY-100635) is a potent and selective 5-HT1A receptor antagonist in a slice preparation of the guinea pig dorsal raphe nucleus: the inhibitory actions on 5-HT neuronal firing of 5-hydroxytryptamine (5-HT, serotonin), 5-carboxamidotryptamine (5-CT) and 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), but not those of baclofen, were abolished by 30 nM WAY-100635. The selective 5-HT1D receptor antagonist N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl) [1,1-biphenyl]-4- carboxamide (GR127935, 300 nM) did not attenuate the 5-HT induced inhibition, indicating that 5-HT1D receptors do not contribute to the inhibitory action of exogenous 5-HT on 5-HT neurones.

引用

页码：R1 / R3

页数：3

共 8 条

[1]

Fletcher A., 1994, British Journal of Pharmacology, V112, p91P

[2] PHARMACOLOGICAL CHARACTERISTICS OF 5-HYDROXYTRYPTAMINE AUTORECEPTORS IN RAT-BRAIN SLICES INCORPORATING THE DORSAL RAPHE OR THE SUPRACHIASMATIC NUCLEUS [J].