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