A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Richard T Lewis, 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

Journal of medicinal chemistry（2006）

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摘要

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.

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