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
收藏
页码：233 / 238
页数：6
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