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.