Recent developments in structure-activity relationships for steroid modulators of GABAA receptors
Recent developments in structure-activity relationships for steroid modulators of GABAA receptors
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DOI：
10.1016/s0165-0173(01)00126-6
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发表时间：
2001-11-01
影响因子：
--
通讯作者：
Purdy, RH
中科院分区：
文献类型：
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作者：
Covey, DF;Evers, AS;Purdy, RH
GABA能神经传递可被类固醇正性和负性调节。类固醇效应被认为是通过类固醇与GABA（A）受体上的特定位点结合来介导的。阳性和阴性调节类固醇的受体位点似乎不同。到目前为止，这些受体上类固醇结合位点的位置和数量尚未确定。在这篇简短的综述中，我们主要集中在我们自己的结构-活性研究的结果。已经研究了新的类似物以进一步描绘化合物通过类固醇结合位点调节受体功能所需的结构特征。已经研究了阳性和阴性调节剂的非天然存在的对映体，以提供受体上存在特异性类固醇结合位点的进一步证据。(C)2001年，爱思唯尔科学。All rights reserved.
GABAergic neurotransmission can be both positively and negatively modulated by steroids. The steroid effects are thought to be mediated by binding of steroids to specific sites on GABA(A) receptors. It appears that the receptor sites for positive and negative modulatory steroids are different. Thus far, the location and number of binding sites for steroids on these receptors have not been established. In this brief review, we concentrate largely on results from our own structure-activity studies. Novel analogues have been studied to further delineate the structural features required for compounds to modulate receptor function via steroid binding sites. Non-naturally occurring enantiomers of both positive and negative modulators have been studied to provide further evidence for the existence of specific steroid binding sites on the receptors. (C) 2001 Elsevier Science BY. All rights reserved.