Methylone and Monoamine Transporters: Correlation with Toxicity
Current Neuropharmacology March 1, 2011 Chiharu Sogawa, Norio Sogawa, Kazumi Ohyama et al. 50 citations
Methylone, a synthetic hallucinogenic amphetamine analog similar to MDMA, inhibits the activity of dopamine, norepinephrine, and serotonin transporters in a concentration-dependent manner, with the strongest effect on the norepinephrine transporter, followed by dopamine and then serotonin transporters. Compared to methamphetamine, methylone is less effective at blocking dopamine and norepinephrine transporters but more effective at blocking the serotonin transporter. Methylone alone is not toxic to cells except at high concentrations, but when combined with methamphetamine, it produces a synergistic toxic effect in cells that express monoamine transporters, likely because methylone acts as a transportable substrate that inhibits transporter function.