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神经甾体在跨膜区2中部的N端一侧的位点作用于γ-氨基丁酸A型(GABA(A))受体。

Neurosteroids act on the GABA(A) receptor at sites on the N-terminal side of the middle of TM2.

作者信息

Rick C E, Ye Q, Finn S E, Harrison N L

机构信息

Department of Anesthesia and Critical Care, Whitman Labs, University of Chicago, IL 60637, USA.

出版信息

Neuroreport. 1998 Feb 16;9(3):379-83. doi: 10.1097/00001756-199802160-00004.

DOI:10.1097/00001756-199802160-00004
PMID:9512375
Abstract

Two sets of chimeras between alphaxalone-sensitive GABA(A) receptor alpha2 or beta1 subunits and the alphaxalone-insensitive glycine receptor alpha1 subunit were constructed to determine the structural domains important for the modulatory actions of neuroactive steroids. These data suggest that the site of action for neurosteroids on GABA(A) receptors is not the same as that for volatile anesthetics and ethanol, but is on the N-terminal side of the middle of TM2.

摘要

构建了两组嵌合体,一组由对alphaxalone敏感的GABA(A)受体α2或β1亚基与对alphaxalone不敏感的甘氨酸受体α1亚基组成,另一组由对alphaxalone不敏感的甘氨酸受体α1亚基与对alphaxalone敏感的GABA(A)受体α2或β1亚基组成,以确定对神经活性类固醇调节作用至关重要的结构域。这些数据表明,神经甾体在GABA(A)受体上的作用位点与挥发性麻醉剂和乙醇的作用位点不同,而是位于跨膜区2中部的N端一侧。

相似文献

1
Neurosteroids act on the GABA(A) receptor at sites on the N-terminal side of the middle of TM2.神经甾体在跨膜区2中部的N端一侧的位点作用于γ-氨基丁酸A型(GABA(A))受体。
Neuroreport. 1998 Feb 16;9(3):379-83. doi: 10.1097/00001756-199802160-00004.
2
Differential subunit dependence of the actions of the general anesthetics alphaxalone and etomidate at gamma-aminobutyric acid type A receptors expressed in Xenopus laevis oocytes.在非洲爪蟾卵母细胞中表达的γ-氨基丁酸A型受体上,全身麻醉药阿法沙龙和依托咪酯作用的亚基依赖性差异。
Mol Pharmacol. 1997 Mar;51(3):484-90.
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A single glycine residue at the entrance to the first membrane-spanning domain of the gamma-aminobutyric acid type A receptor beta(2) subunit affects allosteric sensitivity to GABA and anesthetics.γ-氨基丁酸A型受体β(2)亚基第一个跨膜结构域入口处的单个甘氨酸残基会影响对γ-氨基丁酸和麻醉剂的变构敏感性。
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Comparison of effect of ethanol on N-methyl-D-aspartate- and GABA-gated currents from acutely dissociated neurons: absence of regional differences in sensitivity to ethanol.乙醇对急性分离神经元中N-甲基-D-天冬氨酸门控电流和γ-氨基丁酸门控电流作用的比较:对乙醇敏感性不存在区域差异。
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Subunit mutations affect ethanol actions on GABA(A) receptors expressed in Xenopus oocytes.亚基突变影响乙醇对非洲爪蟾卵母细胞中表达的GABA(A)受体的作用。
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The interaction of general anaesthetics with recombinant GABAA and glycine receptors expressed in Xenopus laevis oocytes: a comparative study.全身麻醉药与非洲爪蟾卵母细胞中表达的重组γ-氨基丁酸A型(GABAA)和甘氨酸受体的相互作用:一项比较研究。
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