| Literature DB >> 11881985 |
Mark S Chambers1, John R Atack, Frances A Bromidge, Howard B Broughton, Susan Cook, Gerard R Dawson, Sarah C Hobbs, Karen A Maubach, Austin J Reeve, Guy R Seabrook, Keith Wafford, Angus M MacLeod.
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.Entities:
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Year: 2002 PMID： 11881985 DOI： 10.1021/jm010471b
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446