Description
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA alpha5 receptor, with an EC50 of 3nM for GABAA alpha5, and Kis of 0.83, 0.85, 0.77and 1.4nM for humanGABAAalpha1beta3gamma2, GABAAalpha2beta3gamma2, GABAAalpha3beta3gamma2, and GABAAalpha5beta3gamma2, respectively; MRK-016 also readily penetrates the CNS