Catalog No.: PC-42117Not For Human Use, Lab Use Only.
MRK-016 (MRK016) is a potent, functionally selective, CNS-penetrating and orally bioavailable inverse agonist of benzodiazepine site of GABAA α5 receptor with Ki of 0.8-1.5 nM for α1-, α2-, α3-, and α5-containing GABAA receptors.
MRK-016 (MRK016) is a potent, functionally selective, CNS-penetrating and orally bioavailable inverse agonist of benzodiazepine site of GABAA α5 receptor with Ki of 0.8-1.5 nM for α1-, α2-, α3-, and α5-containing GABAA receptors.
MRK-016 has inverse agonist efficacy selective for the α5 subtype, increases long-term potentiation in mouse hippocampal slices.
MRK-016 enhances performance in animal models of cognition, does not exhibit the convulsant, proconvulsant, or anxiogenic activity associated with nonselective GABAA inverse agonists.
