Molecular yardsticks. Rigid probes to define the spatial dimensions of the benzodiazepine receptor binding site.
Molecular yardsticks. Rigid probes to define the spatial dimensions of the benzodiazepine receptor binding site.
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分子尺度。
DOI：
10.1021/jm00100a017
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发表时间：
1992
影响因子：
7.3
通讯作者：
Narayanan,K
中科院分区：
文献类型：
--
作者：
Martin,MJ;Trudell,ML;DíazAraúzo,H;Allen,MS;LaLoggia,AJ;Deng,L;Schultz,CA;Tan,YC;Bi,Y;Narayanan,K
自从Librium于1961年被引入，并于1977年发现其通过氨基丁酸(GABA)/苯二氮卓受体（BzR）系统的作用方式以来，苯二氮卓类药物已被广泛使用，很少有其他种类的化合物可以与之媲美。苯二氮卓类激动剂有多种药理作用，但毒性远低于巴比妥类药物。苯二氮卓受体配体通过调节GABA对神经元氯离子通道的门控作用产生药理学作用，最近已证明神经元氯离子通道由至少三种不同的蛋白质组成（,β,）。4-9之前，四聚体蛋白通道管腔被提出（22 ß）；然而,
Introduction Since the introduction of Librium in I9601 andthe subsequent discovery in 1977* 12-3 4567** of its mode of action via the-aminobutyric acid (GABA)/benzodiazepine receptor (BzR) system, the benzodiazepines have enjoyed wide-spread use rivaled by few other classes of compounds. Benzodiazepine agonists effect a variety of pharmacological actions, but are far less toxic than, for example, barbiturates. Benzodiazepine receptor ligands produce their pharmacological effects by modulating the gating action of GABA on neuronal chloride ion channels which have recently been shown to be constituted by at least three distinct proteins (, ß,). 4-9 Previously, a tetrameric protein channel lumen had been proposed (2 2ß); however,