The neurotoxic effects of methylenedioxymethamphetamine (MDMA) and its metabolites on rat brain spheroids in culture

Cell Biol Toxicol. 1999 Jun;15(3):137-42. doi: 10.1023/a:1007658501306.

Abstract

Rat whole-brain spheroids were used to assess the intrinsic neurotoxicity of methylenedioxy-methamphetamine (MDMA, Ecstasy) and two of its metabolites, dihydroxymethamphetamine (DHMA) and 6-hydroxy-MDMA (6-OH MDMA). Exposure of brain spheroids to MDMA or the metabolite 6-OH MDMA (up to 500 micromol/L) for 5 days in culture did not alter intracellular levels of glutathione (GSH), glial fibrillary acidic protein (GFAP) or serotonin (5-HT). In contrast, exposure to the metabolite DHMA, which can deplete intracellular thiols, significantly increased GSH levels (up to 170% of control) following exposure to 50 and 100 micromol/L DHMA. There was also a significant reduction in the levels of glial fibrillary acidic protein (GFAP) and GSH by DHMA at the highest concentration tested (500 micromol/L) but there was no effect on 5HT. This may constitute a sublethal neurotoxic compensatory response to DHMA in an attempt to replenish depleted intraneural GSH levels following metabolite exposure. Rat whole-brain spheroids may thus be a useful in vitro model to delineate mechanisms and effects of this class of neurotoxin.

MeSH terms

  • 3,4-Methylenedioxyamphetamine / analogs & derivatives*
  • 3,4-Methylenedioxyamphetamine / metabolism
  • 3,4-Methylenedioxyamphetamine / toxicity
  • Animals
  • Biomarkers
  • Brain / cytology
  • Brain / drug effects*
  • Brain / enzymology
  • Brain / metabolism
  • Brain Diseases / chemically induced*
  • Brain Diseases / enzymology
  • Brain Diseases / metabolism
  • Cytosol / enzymology
  • Deoxyepinephrine / analogs & derivatives*
  • Deoxyepinephrine / metabolism
  • Deoxyepinephrine / toxicity
  • Dose-Response Relationship, Drug
  • Fetus
  • Glial Fibrillary Acidic Protein / metabolism
  • Glutathione / metabolism
  • L-Lactate Dehydrogenase / metabolism
  • N-Methyl-3,4-methylenedioxyamphetamine / metabolism
  • N-Methyl-3,4-methylenedioxyamphetamine / toxicity*
  • Rats
  • Serotonin / metabolism
  • Serotonin Agents / metabolism
  • Serotonin Agents / toxicity*
  • Spheroids, Cellular / drug effects*

Substances

  • Biomarkers
  • Glial Fibrillary Acidic Protein
  • Serotonin Agents
  • 6-hydroxy-N-methyl-3,4-methylenedioxyamphetamine
  • alpha-methylepinine
  • Serotonin
  • 3,4-Methylenedioxyamphetamine
  • L-Lactate Dehydrogenase
  • Glutathione
  • N-Methyl-3,4-methylenedioxyamphetamine
  • Deoxyepinephrine