Abstract
Esmethadone (dextromethadone; REL-1017) is a novel NMDA receptor (NMDAR) antagonist currently in clinical development for major depressive disorder (MDD). To better understand its role as an NMDAR channel blocker, we examined the functional interaction between REL-1017 and quinolinic acid, an endogenous partial agonist at the glutamate binding site of the NMDAR, and REL-1017 and gentamicin, an antibiotic that modulates NMDAR potentiation.
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