THE NEUROSTEROID DEHYDROEPIANDROSTERONE SULFATE IS AN ALLOSTERIC ANTAGONIST OF THE GABA-A RECEPTOR

被引：401
作者：
MAJEWSKA, MD
DEMIRGOREN, S
SPIVAK, CE
LONDON, ED
机构：
[1] Addiction Research Center, National Institute on Drug Abuse, Baltimore
来源：
BRAIN RESEARCH | 1990年 / 526卷 / 01期
关键词：
Electrophysiology; GABA[!sub]A[!/sub] receptor; Receptor binding; Steroid;
D O I：
10.1016/0006-8993(90)90261-9
中图分类号：
Q189 [神经科学];
学科分类号：
071006 ;
摘要：
Binding of the neurosteroid dehydroepiandrosterone sulfate (DHEAS) to rat brain synaptosomal membranes was studied in vitro, and the interaction of DHEAS with the GABAA receptor was tested using biochemical and electrophysiological assays. DHEAS bound to two populations of sites, and its binding was inhibited by barbiturates. DHEAS interfered with barbiturate-mediated enhancement of benzodiazepine binding. In cultured neurons from ventral mesencephalon, DHEAS reversibly blocked GABA-induced currents, behaving as an allosteric antagonist of the GABAA receptor. © 1990.
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收藏
页码：143 / 146
页数：4
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