Description
Rislenemdaz (MK 0657; CERC 301) is a potent, orally bioavailable, brain-penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1nM and 3.6nM respectively, with no off-target activity; inhibits calcium influx into agonist-stimulatednMDA-GluN1a/GluN2B L (tk-) cells with IC50 of 3.6nM, with no effect on GluN2A up to 30uM; significantly decreases immobility frequency and increases swimming behavior in acute depression models. Depression Phase 2 Clinical