| Literature DB >> 15084116 |
Francine Sternfeld1, Robert W Carling, Richard A Jelley, Tamara Ladduwahetty, Kevin J Merchant, Kevin W Moore, Austin J Reeve, Leslie J Street, Desmond O'Connor, Bindi Sohal, John R Atack, Susan Cook, Guy Seabrook, Keith Wafford, F David Tattersall, Neil Collinson, Gerard R Dawson, José L Castro, Angus M MacLeod.
Abstract
Nonselective inverse agonists at the gamma-aminobutyric acid(A) (GABA-A) benzodiazepine binding site have cognition-enhancing effects in animals but are anxiogenic and can precipitate convulsions. Herein, we describe novel GABA-A alpha5 subtype inverse agonists leading to the identification of 16 as an orally active, functionally selective compound that enhances cognition in animals without anxiogenic or convulsant effects. Compounds of this type may be useful in the symptomatic treatment of memory impairment associated with Alzheimer's disease and related dementias.Entities:
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Year: 2004 PMID： 15084116 DOI： 10.1021/jm031076j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446