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 journalArticle

32 Citations (Scopus)

Abstract

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
Volume9
Issue number1
DOIs
Publication statusPublished - 2011

Fingerprint

Methamphetamine
CHO Cells
Serotonin
GABA Plasma Membrane Transport Proteins
Propane
Dopamine Plasma Membrane Transport Proteins
Poisons
Amphetamine
Norepinephrine
methylone

Keywords

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

ASJC Scopus subject areas

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

Cite this

Sogawa, C., Sogawa, N., Ohyama, K., Kikura-Hanajiri, R., Goda, Y., Sora, I., & Kitayama, S. (2011). Methyl one and monoamine transporters: Correlation with toxicity. Current Neuropharmacology, 9(1), 58-62. https://doi.org/10.2174/157015911795017425

Methyl one and monoamine transporters : Correlation with toxicity. / Sogawa, Chiharu; Sogawa, Norio; Ohyama, Kazumi; Kikura-Hanajiri, Ruri; Goda, Yukihiro; Sora, Ichiro; Kitayama, Shigeo.

In: Current Neuropharmacology, Vol. 9, No. 1, 2011, p. 58-62.

Research output: Contribution to journalArticle

Sogawa, C, Sogawa, N, Ohyama, K, Kikura-Hanajiri, R, Goda, Y, Sora, I & Kitayama, S 2011, 'Methyl one and monoamine transporters: Correlation with toxicity', Current Neuropharmacology, vol. 9, no. 1, pp. 58-62. https://doi.org/10.2174/157015911795017425
Sogawa, Chiharu ; Sogawa, Norio ; Ohyama, Kazumi ; Kikura-Hanajiri, Ruri ; Goda, Yukihiro ; Sora, Ichiro ; Kitayama, Shigeo. / Methyl one and monoamine transporters : Correlation with toxicity. In: Current Neuropharmacology. 2011 ; Vol. 9, No. 1. pp. 58-62.
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