Methyl one and monoamine transporters: Correlation with toxicity

Chiharu Sogawa, Norio Sogawa, Kazumi Ohyama, Ruri Kikura-Hanajiri, Yukihiro Goda, Ichiro Sora, Shigeo Kitayama

Research output: Contribution to journalArticlepeer-review

41 Citations (Scopus)


Methyl one (2-methylamino-1-[3,4-methylenedioxyphenyl]propane-1-one) is a synthetic hallucinogenic amphetamine analog, like MDMA (3,4-methylenedioxy- methamphetamine), considered to act on monoaminergic systems. However, the psychopharmacological profile of its cytotoxicity as a consequence of monoaminergic deficits remains unclear. We examined here the effects of methylone on the transporters for dopamine (DAT), norepinephrine (NET), and serotonin (SERT), using a heterologous expression system in CHO cells, in association with its cytotoxicity. Methylone inhibited the activities of DAT, NET, and SERT, but not GABA transporter-1 (GAT1), in a concentration-dependent fashion with a rank order of NET > DAT > SERT. Methylone was less effective at inhibiting DAT and NET, but more effective against SERT, than was methamphetamine. Methylone alone was not toxic to cells except at high concentrations, but in combination with methamphetamine had a synergistic effect in CHO cells expressing the monoamine transporters but not in control CHO cells or cells expressing GAT1. The ability of methylone to inhibit monoamine transporter function, probably by acting as a transportable substrate, underlies the synergistic effect of methyl one and methamphetamine.

Original languageEnglish
Pages (from-to)58-62
Number of pages5
JournalCurrent Neuropharmacology
Issue number1
Publication statusPublished - 2011
Externally publishedYes


  • Cocaine
  • MDMA
  • Methamphetamine
  • Methylone
  • Neurotransmitter transporter
  • Uptake

ASJC Scopus subject areas

  • Pharmacology
  • Neurology
  • Clinical Neurology
  • Psychiatry and Mental health
  • Pharmacology (medical)


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