含ε亚基的重组人γ-氨基丁酸A（GABA(A)）受体的功能特性
Functional characteristics of recombinant human GABA(A) receptors containing the epsilon-subunit.
作者信息
Thompson S A, Bonnert T P, Whiting P J, Wafford K A
机构信息
Neuroscience Research Centre, Merck Sharp & Dohme Research Laboratories, Harlow, Essex, UK.
出版信息
Toxicol Lett. 1998 Nov 23;100-101:233-8. doi: 10.1016/s0378-4274(98)00190-8.
(1) This paper further examines the functional characteristics of recombinant human GABA(A) receptors containing the epsilon-subunit expressed in Xenopus oocytes. (2) Alpha1beta1epsilon 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 alpha1beta1epsilon and alpha1beta1gamma2s receptors. (4) Direct activation by pentobarbital produced a similar maximum response on alpha1beta1epsilon and alpha1beta1gamma2s, however, both the EC50 and slope were lower on alpha1beta1epsilon compared to alpha1beta1gamma2s. (5) These results describe a novel pharmacology for recombinant alpha1beta1epsilon receptors.
(1) 本文进一步研究了在非洲爪蟾卵母细胞中表达的含ε亚基的重组人γ-氨基丁酸A（GABA(A)）受体的功能特性。(2) α1β1ε受体不受苯二氮䓬类配体或多种下丘脑激素的调节。(3) 静脉麻醉药戊巴比妥、丙泊酚和依托咪酯在α1β1ε和α1β1γ2s受体中均能以相似程度增强亚最大GABA电流（EC20）。(4) 戊巴比妥直接激活在α1β1ε和α1β1γ2s上产生相似的最大反应，然而，与α1β1γ2s相比，α1β1ε上的EC50和斜率均较低。(5) 这些结果描述了重组α1β1ε受体的一种新药理学特性。
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