Document Report Card

ID: ALA1135580

Journal: J Med Chem

Title: 6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.

Authors: Chambers MS, Atack JR, Bromidge FA, Broughton HB, Cook S, Dawson GR, Hobbs SC, Maubach KA, Reeve AJ, Seabrook GR, Wafford K, MacLeod AM.

Abstract: Nonselective inverse agonists at the benzodiazepine binding site on the GABA-A chloride ion channel enhance cognitive performance in animals but cannot be used in the treatment of cognitive disorders because of anxiogenic and convulsant side effects. We have identified a novel series of GABA-A alpha5 receptor ligands during our search for alpha5 receptor inverse agonists as potential cognition enhancers. In particular, 6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5H)-one (26) has been identified as a functionally selective GABA-A alpha5 inverse agonist.

CiteXplore: 11881985

DOI: 10.1021/jm010471b