| Literature DB >> 16392789 |
Simon C Goodacre1, Leslie J Street, David J Hallett, James M Crawforth, Sarah Kelly, Andrew P Owens, Wesley P Blackaby, Richard T Lewis, Joanna Stanley, Alison J Smith, Pushpinder Ferris, Bindi Sohal, Susan M Cook, Andrew Pike, Nicola Brown, Keith A Wafford, George Marshall, José L Castro, John R Atack.
Abstract
A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.Entities:
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Year: 2006 PMID： 16392789 DOI： 10.1021/jm051065l
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446