Synthesis, in Vitro Affinity, and Efficacyof a Bis 8-Ethynyl-4H-imidazo[1,5a]-[1,4]benzodiazepine Analogue, the FirstBivalent α5 Subtype Selective BzR/GABAA Antagonist
The synthesis and in vitro affinity of the α5β3γ2(α5) subtype selective BzR/GABAA antagonist 7 is described.This ligand is selective for α5 subtypes in vitro and is a potentantagonist of the effects of diazepam only at α5β3γ2 subtypes(oocytes). Ligands such as 7 will be important in the determination of which physiological function(s) are subserved bythis GABAA α5 subtype.
