KRM-II-81 is a selective α2/α3 subtype GABAA receptor ligand (positive allosteric modulator) with EC50 of 937 nM for α3β3γ2 GABAAR.
KRM-II-81 demonstrated similar efficacy at α1/α2/α3 GABAA receptors and negligible efficacy at α4/α5/α6 GABAA receptors, with α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits.
KRM-II-81 exhibited improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.
KRM-II-81 dose-dependently decreased 0.6% acetic acid- and 0.32% lactic acid-induced writhing.
KRM-II-81 exhibited significant antinociceptive effects in chemical stimulation-induced pain in mice.
