Drug intelligence / Profile preview

methylone

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral, Intranasal, Intravenous, Inhalation, Rectal
01

Overview

Methylone is a synthetic cathinone and entactogen structurally related to MDMA (3,4-methylenedioxymethamphetamine), often described as its beta-keto analog. It acts primarily as a substrate for monoamine transporters—dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT)—promoting the release of dopamine, norepinephrine, and serotonin into the synaptic cleft. This results in stimulant and empathogenic effects similar to those of MDMA but with some pharmacological differences; notably methylone releases less dopamine than MDMA but comparable levels of norepinephrine and serotonin[2][3][6]. Preclinical studies suggest rapid-acting antidepressant- and anxiolytic-like effects in animal models[7], with emerging interest in its potential for treating major depressive disorder (MDD) and post-traumatic stress disorder (PTSD)[8]. Methylone is not approved for medical use; it has been used recreationally as a "designer drug" or "bath salt" substitute for MDMA[1][5].

Other names
methylone3,4-methylenedioxy-N-methylcathinoneMDMCβk-MDMAM1M-1M 1
02

Targets

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

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