6,7-Dihydro-2-benzothiophen-4(5H)-ones: A Novel Class of GABA-A α5 Receptor Inverse Agonists
- 12 February 2002
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 45 (6) , 1176-1179
- https://doi.org/10.1021/jm010471b
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 α5 receptor ligands during our search for α5 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 α5 inverse agonist.Keywords
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