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

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

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...

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Veröffentlicht in:Brain research 1990-08, Vol.526 (1), p.143-146
Hauptverfasser: Majewska, M D, Demirgören, S, Spivak, C E, London, E D
Format: Artikel
Sprache:eng
Schlagworte:
Allosteric Regulation - drug effects
Animals
Dehydroepiandrosterone - analogs & derivatives
Dehydroepiandrosterone - metabolism
Dehydroepiandrosterone - pharmacology
Dehydroepiandrosterone Sulfate
GABA-A Receptor Antagonists
In Vitro Techniques
Intracellular Membranes - drug effects
Male
Rats
Rats, Inbred F344
Steroids - metabolism
Synaptosomes - drug effects
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Zusammenfassung: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.
ISSN:0006-8993
DOI:10.1016/0006-8993(90)90261-9