Functional characteristics of recombinant human GABAA receptors containing the ε-subunit

被引：21

作者：

Thompson, SA ^{[1
]}

Bonnert, TP ^{[1
]}

Whiting, PJ ^{[1
]}

Wafford, KA ^{[1
]}

机构：

[1] Merck Sharp & Dohme Ltd, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

来源：

TOXICOLOGY LETTERS | 1998年 / 101卷

关键词：

GABA; epsilon-subunit; Xenopus oocytes; anaesthetic agents; benzodiazepines;

D O I：

10.1016/S0378-4274(98)00190-8

中图分类号：

R99 [毒物学（毒理学）];

学科分类号：

100405 ;

摘要：

(1) This paper Further examines the functional characteristics of recombinant human GABA(A) receptors containing the epsilon-subunit expressed in Xenopus oocytes. (2) alpha 1 beta 1 epsilon receptors are not modulated by benzodiazepine ligands or by a number of hypothalamic hormones. (3) The intravenous anaesthetic agents pentobarbital, propofol and etomidate all potentiate sub-maximal GABA currents (EC20) to a similar degree in alpha 1 beta 1 epsilon and alpha 1 beta 1 gamma 2s receptors. (4) Direct activation by pentobarbital produced a similar maximum response on alpha 1 beta 1 epsilon and alpha 1 beta 1 gamma 2s, however, both the EC50 and slope were lower on alpha 1 beta 1 epsilon compared to alpha 1 beta 1 gamma 2s. (5) These results describe a novel pharmacology for recombinant alpha 1 beta 1 epsilon receptors. (C) 1998 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：233 / 238

页数：6