Esmethadone (Rel-1017) Restores Nmda Receptor 1 Subunit Expression In An In Vitro Model Of Glutamatergic Excitotoxicity

Esmethadone (dextromethadone; REL-1017) is a novel NMDA channel blocker currently in development for major depressive disorder (MDD). NMDA receptors are known to play a primary role in neural plasticity. An excess of glutamate in the synaptic cleft and impaired neural plasticity have been implicated in the pathogenesis of MDD. The NMDA receptor 1 subunit (NMDAR1) is essential for NMDA receptor membrane expression. To gain insight into the mechanism of action of REL-1017, we examined the effect of glutamate and REL-1017 on the expression of NMDAR1 in ARPE-19 cells.