RO 4938581

RO 4938581 is a potent and selective GABA_A α5 inverse agonist, with a K_i of 4.6 nM for GABA_A α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (K_i, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction. IC50 & Target: Ki: 4.6 nM (GABA_A α5β3γ2a), 174 nM (GABA_A α1β3γ2a), 185 nM (GABA_A α2β3γ2a), 80 nM (GABA_A α3β3γ2a)^[1] In Vitro: RO 4938581 is a potent and selective GABA_A α5 inverse agonist, with a K_i of 4.6 nM for GABA_A α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (K_i, 174, 185, 80 nM, respectively)^[1]. In Vivo: RO 4938581 (0.3-1 mg/kg, p.o.) reverses a working memory impairment induced by scopolamine the delayed match to position (DMTP) task and a spatial learning impairment induced by diazepam (RO 4938581; 1-10 mg/kg, po)^[1].