KRM-II-81

KRM-II-81 is a potent, selective α1/α2/α3 GABAA receptors positive allosteric modulator with EC50 of 937 nM for α1β3γ2, negligible efficacy at α4/α5/α6 GABAA receptors; shows 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.

References 1. Poe MM, et al. J Med Chem. 2016 Dec 8;59(23):10800-10806. 2. Lewter LA, et al. ACS Chem Neurosci. 2017 Jun 21;8(6):1305-1312. View Related Products by Target GABA Receptor