Biochem/physiol Actions MRK-016 is an orally active, benzodiazepine site-targeting, alpha5-selective GABAA inverse agonist (Emax = -55%/α:5, -16%/α:1, -9%/α:3, +6%/α:2 of a EC20 GABA response using respective recombinant human
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MRK-016 is an orally active, benzodiazepine site-targeting, alpha5-selective GABAA inverse agonist (Emax = -55%/α5, -16%/α1, -9%/α3, +6%/α2 of a EC20 GABA response using respective recombinant human αβ3γ2) with in vivo cognition-enhancing properties (0.3-3 mg/kg p.o. in rat Morris water maze test).
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