375857-62-8Relevant articles and documents
Discovery of imidazo[1,2-b][1,2,4]triazines as GABAA α2/3 subtype selective agonists for the treatment of anxiety
Russell, Michael G. N.,Carling, Robert W.,Street, Leslie J.,Hallett, David J.,Goodacre, Simon,Mezzogori, Elena,Reader, Michael,Cook, Susan M.,Bromidge, Frances A.,Newman, Robert,Smith, Alison J.,Wafford, Keith A.,Marshall, George R.,Reynolds, David S.,Dias, Rebecca,Ferris, Pushpindar,Stanley, Jo,Lincoln, Rachael,Tye, Spencer J.,Sheppard, Wayne F. A.,Sohal, Bindi,Pike, Andrew,Dominguez, Maria,Atack, John R.,Castro, José L.
, p. 1235 - 1238 (2007/10/03)
The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABAA α3-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.
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABAAα2/α3 binding site agonists for the treatment of anxiety disorders
Goodacre, Simon C.,Street, Leslie J.,Hallett, David J.,Crawforth, James M.,Kelly, Sarah,Owens, Andrew P.,Blackaby, Wesley P.,Lewis, Richard T.,Stanley, Joanna,Smith, Alison J.,Ferris, Pushpinder,Sohal, Bindi,Cook, Susan M.,Pike, Andrew,Brown, Nicola,Wafford, Keith A.,Marshall, George,Castro, José L.,Atack, John R.
, p. 35 - 38 (2007/10/03)
A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA Aα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.