Document Report Card

ID: ALA1146597

Journal: J Med Chem

Title: Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.

Authors: Li X, Cao H, Zhang C, Furtmueller R, Fuchs K, Huck S, Sieghart W, Deschamps J, Cook JM.

Abstract: The synthesis and in vitro affinity of the alpha5beta3gamma2 (alpha5) subtype selective BzR/GABA(A) antagonist 7 is described. This ligand is selective for alpha5 subtypes in vitro and is a potent antagonist of the effects of diazepam only at alpha5beta3gamma2 subtypes (oocytes). Ligands such as 7 will be important in the determination of which physiological function(s) are subserved by this GABA(A) alpha5 subtype.

CiteXplore: 14667209

DOI: 10.1021/jm034164c