Chemical Name:6,7-Dihydro-3-[(2-hydroxyethyl)thio]-6,6-dimethyl-1-(2-
thiazolyl)-benzo[c]thiophen-4(5H)-one
Biological Activity:
GABAA receptor inverse agonist
selective for the α5-subtype
(Ki values are 1.6, 16, 20 and 20 nM for α5, α2, α1 and α3 subtypes
respectively). Brain penetrant; enhances cognitive performance in rats in the
delayed matching-to-place morris water maze test following i.p. administration.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.