A Pyridazine Series of α2/α3 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 GABAA α2/α3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably α3-selective compound ideal for in vivo study. These ligands are antagonists at the α1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability.

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α2/α3 subtype selective gaba<sub>a</sub>,pyridazine series,anxiety

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A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety

A Pyridazine Series of α2/α3 Subtype Selective GABA_A Agonists for the Treatment of Anxiety