Effect of amphetamine on extrastriatal D2 dopamine receptor binding in the primate brain: A PET study

Toni S. Shippenberg, William Rea, Barbara S. Slusher

Research output: Contribution to journalArticlepeer-review

58 Scopus citations


[11C]raclopride binding to D2 dopamine receptors in the striatum is sensitive to drug-induced changes of endogenous dopamine concentration. We recently developed the new radioligand [11C]FLB 457, which is suitable for positron emission tomography (PET) studies of extrastriatal D2 dopamine receptors. The purpose of this PET study was to examine the effect of amphetamine on [11C]FLB 457 binding in extrastriatal regions. Each of three cynomolgus monkeys was examined at baseline conditions, 15 min and 3 h after I.V. injection of amphetamine (2 mg/kg). The effect of amphetamine was calculated from the ratio of specific [11C]FLB 457 binding to the binding in the cerebellum, a region which was used as reference for free and nonspecific binding in the brain. The changes of the ratio in the striatum, the thalamus, and the neocortex were between -1.2% and -15.5% at 15 min and -2.1% and -16.3% at 3 h, respectively, after amphetamine administration. The reductions of the binding ratios in the extrastriatal regions are similar to those reported for [11C]raclopride binding in the striatum. These data in a limited series of monkeys suggest that [11C]FLB 457 binding to D2 dopamine receptors in extrastriatal regions is sensitive to changes in the concentration of endogenous dopamine. (C) 2000 Wiley-Liss, Inc.

Original languageEnglish (US)
Pages (from-to)138-143
Number of pages6
Issue number2
StatePublished - Oct 30 2000
Externally publishedYes


  • Amphetamine
  • D2 dopamine receptor
  • Endogenous dopamine
  • Positron emission tomography (PET)
  • [C]FLB 457

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience


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