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[γ-氨基丁酸受体氯离子通道]

[GABA receptor chloride ion channel].

作者信息

Hashimoto T

机构信息

Department of Pharmacology, Kyoto Prefectural University of Medicine.

出版信息

Nihon Rinsho. 1998 Jul;56(7):1824-9.

PMID:9702060
Abstract

Gamma-Aminobutyric acid(GABA) has been established as a major inhibitory neurotransmitter in the brain. GABAA receptors are coupled to benzodiazepine receptors and barbiturate binding site. They are ligand-gated Cl- channels that consist of a heteromeric mixture of protein subunits forming a pentameric structure. On the other hand, GABAC receptors appear to be relatively simple ligand-gated Cl- channels with a distinctive pharmacology, in that they are not blocked by bicuculline and not modulated by barbiturates, benzodiazepines or neuroactive steroids. Therefore, it is suggested that these multiple GABA receptors generate various inhibitory functions and the pharmacology of these novel subtypes of GABA receptors may yield important therapeutic agents.

摘要

γ-氨基丁酸(GABA)已被确认为大脑中的一种主要抑制性神经递质。GABAA受体与苯二氮䓬受体和巴比妥类结合位点相连。它们是配体门控氯离子通道,由形成五聚体结构的蛋白质亚基异源混合物组成。另一方面,GABAC受体似乎是相对简单的配体门控氯离子通道,具有独特的药理学特性,即它们不会被荷包牡丹碱阻断,也不会被巴比妥类、苯二氮䓬类或神经活性甾体调节。因此,有人提出这些多种GABA受体产生各种抑制功能,并且这些新型GABA受体亚型的药理学特性可能会产生重要的治疗药物。

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