Document Report Card

ID: ALA1146073

Journal: J Med Chem

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

Authors: Lewis RT, Blackaby WP, Blackburn T, Jennings AS, Pike A, Wilson RA, Hallett DJ, Cook SM, Ferris P, Marshall GR, Reynolds DS, Sheppard WF, Smith AJ, Sohal B, Stanley J, Tye SJ, Wafford KA, Atack JR.

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.

CiteXplore: 16610803

DOI: 10.1021/jm051144x