作者
Michael G. N. Russell,Robert W. Carling,Leslie J. Street,David J. Hallett,Simon Goodacre,Elena Mezzogori,Michael Reader,Susan M. Cook,Frances A. Bromidge,Robert Newman,Alison J. Smith,Keith A. Wafford,George Marshall,D. S. Reynolds,Rebecca Dias,Pushpindar Ferris,John C. Stanley,Rachael J. Lincoln,Spencer J. Tye,Wayne F. A. Sheppard,Bindi Sohal,Andy Pike,M.Á. Domínguez,John Atack,José L. Castro
摘要
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.