Xli 093 is an α5 subtype selective benzodiazepine/GABAA receptor antagonist. Xli 093 shows Ki = 5 nM at the α5 receptor in Ltk- cell membranes expressing human α5β3γ2 receptors; little or no affinity at other BDZ/ GABAA subtypes; does not trigger chloride currents in any subtype of tested subtypes, up to 1 μM in concentration; dose-dependently and completely inhibits diazepam stimulated currents in α5β3γ2 receptors.
Li, X., et al., Synthesis, in vitro affinity and efficacy of a Bis 8-ethynyl-4H-imidazo[1,5a]-[1,4]benzodiazepine analogue, the first bivalent a5 subtype selective BzR/ GABAA antagonist. J. Med. Chem. 46, 5567-5570, (2003)