Repeated administration of the substituted amphetamine p-methoxyamphetamine produces reductions in cortical 5-HT transporter binding but not 5-HT content, unlike 3,4-methylenedioxyamethamphetamine

Eur J Pharmacol. 2006 Sep 28;546(1-3):74-81. doi: 10.1016/j.ejphar.2006.07.011. Epub 2006 Jul 25.

Abstract

Worldwide growth in p-methoxyamphetamine (PMA) usage amongst 'ecstasy' users indicates a proportionally greater incidence of acute toxicity compared to 3,4-methylenedioxymethamphetamine (MDMA). While longer-term use of MDMA appears to produce degeneration of 5-hydroxytryptamine (5-HT, serotonin) neurons, PMA effects are poorly understood. The aim of this study was to determine the effect of repeated PMA administration on two indices of 5-HT axonal degeneration, cortical brain 5-HT transporter (SERT) density and 5-HT/5-hydroxyindolacetic acid (5-HIAA) content. Treatment of male rats once daily for 4 days (10 or 20 mg/kg) with PMA or MDMA resulted in significant reductions (20 mg/kg: 53% and 23% of vehicle treatment respectively) in [(3)H]-paroxetine binding (SERT density) one week after final drug administration. When rats were housed at a higher ambient temperature (28 degrees C vs. 22 degrees C) for 6 h after dosing, no additive effect was seen for either drug. A more intensive dosing regimen (10 or 20 mg/kg twice daily for 4 days) was used to examine PMA/MDMA effects on cortical 5-HT content. Two weeks after MDMA treatment, significant reductions in cortical 5-HT content (20 mg/kg: 39% of vehicle treatment) were seen. However, PMA did not alter cortical 5-HT content, yet reduced cortical 5-HIAA content (20 mg/kg: 72% of vehicle treatment). These data suggest PMA has severe long-term implications clinically for alteration of 5-HT neurotransmission that may differ from MDMA, but may not necessarily be interpreted as a degeneration of 5-HT fibres.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3,4-Dihydroxyphenylacetic Acid / metabolism
  • Amphetamines / metabolism
  • Amphetamines / pharmacology*
  • Animals
  • Binding, Competitive
  • Brain Chemistry / drug effects
  • Cerebral Cortex / drug effects*
  • Cerebral Cortex / metabolism
  • Chromatography, High Pressure Liquid
  • Dopamine / metabolism*
  • Dose-Response Relationship, Drug
  • Electrochemistry
  • Hallucinogens / metabolism
  • Hallucinogens / pharmacology*
  • Hydroxyindoleacetic Acid / metabolism
  • Male
  • N-Methyl-3,4-methylenedioxyamphetamine / metabolism
  • N-Methyl-3,4-methylenedioxyamphetamine / pharmacology*
  • Paroxetine / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Selective Serotonin Reuptake Inhibitors / metabolism
  • Serotonin / metabolism
  • Serotonin Plasma Membrane Transport Proteins / drug effects*
  • Serotonin Plasma Membrane Transport Proteins / metabolism
  • Synaptic Transmission / drug effects
  • Time Factors

Substances

  • Amphetamines
  • Hallucinogens
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin Uptake Inhibitors
  • 3,4-Dihydroxyphenylacetic Acid
  • Serotonin
  • Paroxetine
  • Hydroxyindoleacetic Acid
  • N-Methyl-3,4-methylenedioxyamphetamine
  • 4-methoxyamphetamine
  • Dopamine