Document Report Card

ID: ALA1149444

Journal: J Med Chem

Title: Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

Authors: Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL.

Abstract: The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABA(A) alpha3-containing receptor subtype is described, leading to the identification of a clinical candidate, 11. Compound 11 shows good bioavailability and half-life in preclinical species, and it is a nonsedating anxiolytic in both rat and squirrel monkey behavioral models.

CiteXplore: 16480260

DOI: 10.1021/jm051200u