Influence of a low dose of amphetamine on vesicular monoamine transporter binding: a PET (+)[11C]DTBZ study in humans

Synapse. 2010 Jun;64(6):417-20. doi: 10.1002/syn.20743.

Abstract

We previously reported increased binding of (+)[11C]DTBZ (dihydrotetrabenazine), the vesicular monoamine transporter (VMAT2) positron emission tomography (PET) radioligand, in striatum of some methamphetamine users. This finding might be explained by stimulant-induced vesicular DA depletion resulting in decreased DA (+)[11C]DTBZ competition at VMAT2. In a prospective PET study, we now find that administration of an acute oral dose of amphetamine (0.4 mg/kg) to humans does not cause increased striatal (+)[11C]DTBZ binding but a slight 5% decrease. Our data suggest that a low amphetamine dose is unlikely to cause sufficient DA depletion to detect increased (+)[11C]DTBZ binding and that a higher dose might be required.

MeSH terms

  • Administration, Oral
  • Adult
  • Amphetamine / pharmacology*
  • Amphetamine-Related Disorders / metabolism
  • Amphetamine-Related Disorders / physiopathology
  • Binding, Competitive / drug effects
  • Binding, Competitive / physiology
  • Central Nervous System Stimulants / pharmacology
  • Corpus Striatum / diagnostic imaging
  • Corpus Striatum / drug effects*
  • Corpus Striatum / metabolism
  • Dopamine / metabolism
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Male
  • Positron-Emission Tomography / methods*
  • Prospective Studies
  • Tetrabenazine / analogs & derivatives*
  • Tetrabenazine / metabolism
  • Vesicular Monoamine Transport Proteins / drug effects*
  • Vesicular Monoamine Transport Proteins / metabolism
  • Young Adult

Substances

  • Central Nervous System Stimulants
  • SLC18A2 protein, human
  • Vesicular Monoamine Transport Proteins
  • dihydrotetrabenazine
  • Amphetamine
  • Dopamine
  • Tetrabenazine