Drug modulation of GABAA-mediated transmission

Abstract Synaptic transmission mediated by GABAA receptors is a target for a variety of centrally acting anticonvulsant, anxiolytic, sedative-hypnotic and convulsant drugs. Picrotoxin, a non-competitive antagonist of GABA, binds to a distinct site on the oligomeric complex and is allosterically coupled to GABA, benzodiazepine, barbiturate and steroid sites. Recent studies have shown that the picrotoxin site can be modulated both positively and negatively, in a manner analogous to the benzodiazepine receptor sites.

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