GluN2A PAM Y36 is a potent, GluN2A-selective N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulator with EC50 of 24.97 uM, Emax=397.7%.
Y36 showed higher efficacy (Emax = 397.7%) than GNE-3419 (Emax = 196.4%), reducing the EC50 values and increasing the Emax values for glutamate/glycine at GluN2A receptor.
Y36 significantly alleviated depression-related behaviors in multiple behavioral assessments in chronic restraint stress (CRS) mice.
Y36 has favorable pharmacokinetic (PK) profiles and blood-brain barrier (BBB) penetration, with no signs of addiction, weight gain, or organ and tissue damage in mice.
