REL-1017 (esmethadone) Showed No Reinforcing Properties Compared to Oxycodone in Rat Self-Administration Study

Henningfield J, Gauvin D, Bifari F, Fant R, Caron J, Buchhalter A, Ashworth J, Pappagallo M, Folli F, Manfredi PL

REL-1017 (esmethadone; dextromethadone) is an NMDAR channel blocker with a preference for hyperactive channels and has twenty-fold lower activity at the μ(mu)-opioid receptor than racemic methadone. REL-1017 is being developed for treatment of Major Depressive Disorder. The purpose of this study was to evaluate the potential reinforcing effects of REL-1017 compared to oxycodone in an intravenous (IV) rat selfadministration study.

Presented at the College on Problems of Drug Dependence 83rd Annual Scientific Virtual Meeting, June 21–24, 2021