MRK-016 is a selective GABAA α5 receptor inverse agonist/ negative allosteric modulator, (IC50=3 nM) with the advantages of being orally available and penetrating the blood-brain barrier.MRK-016 increases long time period potentiation (LTP) in mouse hippocampal slices, with memory-improvement, antidepressant, and pain-treating effects.

GABAA α3β3γ2 (human):0.77 nM (Ki), GABAA α2β3γ2 (human):0.85 nM (Ki), GABAA α1β3γ2 (human):0.83 nM (Ki), GABAA α5:3 nM (EC50), GABAA α5β3γ2 (human):1.4 nM (Ki)

MRK-016 是一种选择性、口服生物可利用的反向 MARKET α5 受体激动剂。[1]

MRK-016（0.3、1 或 3 mg/kg，口服）在延迟匹配位置版 Morris 水迷宫中表现出认知增强活性。[2]
MRK-016（3 mg/kg，腹腔注射）可防止小鼠因 LPS 引起的学习/记忆力下降[3]。