| Literature DB >> 15026049 |
James Crawforth1, John R Atack, Susan M Cook, Karl R Gibson, Alan Nadin, Andrew P Owens, Andrew Pike, Michael Rowley, Alison J Smith, Bindi Sohal, Francine Sternfeld, Keith Wafford, Leslie J Street.
Abstract
A series of tricyclic pyridones has been evaluated as benzodiazepine site ligands with functional selectivity for the alpha(3) over the alpha(1) containing subtype of the human GABA(A) receptor ion channel. This investigation led to the identification of a high affinity, functionally selective, orally bioavailable benzodiazepine site ligand that demonstrated activity in rodent anxiolysis models and reduced sedation relative to diazepam.Entities:
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Year: 2004 PMID： 15026049 DOI： 10.1016/j.bmcl.2004.01.057
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823