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).
Orally active, benzodiazepine site-targeting, alpha5 (α5) subtype-selective GABAA inverse agonist with cognition-enhancing properties in vivo.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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α5-containing GABAARs are potential therapeutic targets for clinical conditions including age-related dementia, stroke, schizophrenia, Down syndrome, anaesthetic-induced amnesia, anxiety and pain. α5-containing GABAARs are expressed in layer 5 cortical neurons and hippocampal pyramidal neurons where they mediate both tonic currents
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