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Methylone and monoamine transporters: correlation with toxicity

Chiharu Sogawa1, Norio Sogawa, Kazumi Ohyama

  • 1Department of Dental Pharmacology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 2-5-1 Shikata-cho, Okayama 700-8525, Japan.

Current Neuropharmacology
|September 3, 2011
PubMed

Insights

Methylone, a synthetic amphetamine, inhibits dopamine, norepinephrine, and serotonin transporters. It synergistically increases methamphetamine toxicity in cells expressing these transporters, likely by acting as a substrate.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Toxicology

Background:

  • Methylone is a synthetic amphetamine analog with effects on monoaminergic systems.
  • The cytotoxicity of methylone, particularly concerning monoaminergic deficits, is not fully understood.

Purpose of the Study:

  • To investigate the effects of methylone on dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters.
  • To assess the cytotoxicity of methylone, alone and in combination with methamphetamine, in cells expressing monoamine transporters.

Main Methods:

  • Utilized a heterologous expression system in Chinese hamster ovary (CHO) cells.
  • Assessed transporter inhibition by methylone and methamphetamine.
  • Evaluated cytotoxicity in control CHO cells, cells expressing monoamine transporters, and cells expressing GABA transporter-1 (GAT1).

Main Results:

  • Methylone inhibited DAT, NET, and SERT activity in a concentration-dependent manner (NET > DAT > SERT).
  • Methylone showed greater potency against SERT inhibition compared to methamphetamine.
  • Methylone potentiated methamphetamine-induced cytotoxicity synergistically in cells expressing monoamine transporters, but not in control cells or GAT1-expressing cells.

Conclusions:

  • Methylone's inhibition of monoamine transporter function contributes to its psychopharmacological profile.
  • Methylone likely acts as a transportable substrate, enhancing the synergistic toxicity observed with methamphetamine.
Keywords:
MDMA.Methylonecocainemethamphetamineneurotransmitter transporteruptake

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