Drug intelligence / Profile preview

R-methylone

Development stage
Preclinical
Lead developer
Transcend Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

R-methylone is the (R)-enantiomer of methylone (3,4-methylenedioxy-N-methylcathinone), a synthetic cathinone and phenethylamine derivative that acts as an entactogen and stimulant. It functions as a triple monoamine releasing agent and reuptake inhibitor, increasing the synaptic concentrations of serotonin, norepinephrine, and dopamine by interacting with their respective transporters (SERT, NET, and DAT). While racemic methylone is being developed under the code TSND-201 by Transcend Therapeutics for the treatment of Post-Traumatic Stress Disorder (PTSD), the (R)-enantiomer is specifically noted for its distinct pharmacological profile. In many cathinones and related phenethylamines, the (R)-enantiomer often exhibits a different balance of monoamine release compared to the (S)-enantiomer, potentially offering a more favorable therapeutic window by reducing stimulant-related side effects while maintaining prosocial or entactogenic benefits. It is currently being explored in the context of psychedelic-assisted therapies for neuropsychiatric conditions.

Other names
(R)-methylone(R)-3,4-methylenedioxy-N-methylcathinone(R)-bk-MDMA
02

Targets

SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)

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