Imidazo[1,2-b][1,2,4]triazines as α2/α3 subtype selective GABAA agonists for the treatment of anxiety

Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABAA receptors that are functionally selective for the α2/α3 subtypes over the α1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described.

Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABAA receptors that are functionally selective for the α2/α3 subtypes over the α1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described.Figure optionsDownload as PowerPoint slide