(+/-)-3,4-Methylenedioxymethamphetamine administration to rats does not decrease levels of the serotonin transporter protein or alter its distribution between endosomes and the plasma membrane

J Pharmacol Exp Ther. 2005 Sep;314(3):1002-12. doi: 10.1124/jpet.105.088476. Epub 2005 Jun 3.

Abstract

We showed that the serotonin (5-HT) neurotoxin 5,7-dihydroxytryptamine (5,7-DHT) reduces brain tissue 5-HT, decreases expression of 5-HT transporter (SERT) protein, and increases expression of glial fibrillary acidic protein (GFAP). In contrast, doses of (+/-)-3,4-methylenedioxymethamphetamine (MDMA) that decrease brain tissue 5-HT fail to alter expression of SERT or GFAP. Using a new and highly sensitive anti-SERT antibody, we determined whether MDMA alters the subcellular distribution of SERT protein by measuring SERT expression in endosomes and plasma membranes 2 weeks after MDMA administration. Rat brain tissues (caudate, cortex, and hippocampus) were collected 3 days and 2 weeks after MDMA (7.5 mg/kg i.p., every 2 h x 3 doses) or 5,7-DHT (150 microg/rat i.c.v.) administration. Representative results from cortex are as follows. At both 3 days and 2 weeks postinjection, MDMA decreased tissue 5-HT (65%) and had no effect on GFAP expression. MDMA increased heat shock protein 32 (HSP32; a marker for microglial activation) expression (30%) at 3 days, but not 2 weeks. MDMA did not alter SERT expression at either time point and did not alter SERT levels in either endosomes or plasma membranes (2 weeks). 5,7-DHT decreased tissue 5-HT (80%), increased HSP32 expression at both time points (about 50%), and increased GFAP expression at 2 weeks (40%). 5,7-DHT decreased SERT expression (33%) at 2 weeks, but not at 3 days. These findings indicate that a dosing regimen of MDMA that depletes brain 5-HT does not alter SERT protein expression or the distribution of SERT between endosomes and the plasma membrane and does not produce detectable evidence for neurotoxicity.

MeSH terms

  • 5,7-Dihydroxytryptamine / pharmacology
  • Animals
  • Cell Membrane / chemistry*
  • Endosomes / chemistry*
  • Glial Fibrillary Acidic Protein / analysis
  • Heme Oxygenase (Decyclizing) / analysis
  • Male
  • Membrane Glycoproteins / analysis
  • Membrane Glycoproteins / drug effects*
  • Membrane Glycoproteins / metabolism
  • Membrane Transport Proteins / analysis
  • Membrane Transport Proteins / drug effects*
  • Membrane Transport Proteins / metabolism
  • N-Methyl-3,4-methylenedioxyamphetamine / pharmacology*
  • Nerve Tissue Proteins / analysis
  • Nerve Tissue Proteins / drug effects*
  • Nerve Tissue Proteins / metabolism
  • Neuroglia / chemistry
  • Neurons / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Serotonin / analysis
  • Serotonin Plasma Membrane Transport Proteins

Substances

  • Glial Fibrillary Acidic Protein
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Serotonin Plasma Membrane Transport Proteins
  • Slc6a4 protein, rat
  • 5,7-Dihydroxytryptamine
  • Serotonin
  • Heme Oxygenase (Decyclizing)
  • Hmox1 protein, rat
  • N-Methyl-3,4-methylenedioxyamphetamine