Description: | MRK-016 is a selective, orally bioavailable inverse agonist of GABAA ?5 receptor, with an EC50 of 3 nM for GABAA ?5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA??1?3?2, GABAA??2?3?2, GABAA??3?3?2, and GABAA??5?3?2, respectively; MRK-016 also readily penetrates the CNS. |