The neurosteroid dehydroepiandrosterone sulfate is an allosteric antagonist of the GABAA receptor

作者: Maria Dorota Majewska , Serdar Demirgo¨ren , Charles E. Spivak , Edythe D. London

DOI: 10.1016/0006-8993(90)90261-9

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摘要: Binding of the neurosteroid dehydroepiandrosterone sulfate (DHEAS) to rat brain synaptosomal membranes was studied in vitro, and interaction DHEAS with GABAA receptor tested using biochemical electrophysiological assays. bound two populations sites, its binding inhibited by barbiturates. interfered barbiturate-mediated enhancement benzodiazepine binding. In cultured neurons from ventral mesencephalon, reversibly blocked GABA-induced currents, behaving as an allosteric antagonist receptor.

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