| Literature DB >> 16610803 |
Richard T Lewis1, Wesley P Blackaby, Timothy Blackburn, Andrew S R Jennings, Andrew Pike, Rowan A Wilson, David J Hallett, Susan M Cook, Pushpinder Ferris, George R Marshall, David S Reynolds, Wayne F A Sheppard, Alison J Smith, Bindi Sohal, Joanna Stanley, Spencer J Tye, Keith A Wafford, John R Atack.
Abstract
The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selective compound ideal for in vivo study. These ligands are antagonists at the alpha1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability.Entities:
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Year: 2006 PMID： 16610803 DOI： 10.1021/jm051144x
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446