MRK-016 is a selective, orally bioavailable inverse agonist of GABA A α5 receptor , with an EC 50 of 3 nM for GABA A α5, and K i s of 0.83, 0.85, 0.77 and 1.4 nM for human GABA A α1β3γ2, GABA A α2β3γ2, GABA A α3β3γ2, and GABA A α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
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