Date: 05 Nov 2008

The effects of d-amphetamine on extrastriatal dopamine D2/D3 receptors: a randomized, double-blind, placebo-controlled PET study with [11C]FLB 457 in healthy subjects

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Abstract

Purpose

The dopamine D2/D3 receptor ligand [11C]FLB 457 and PET enable quantification of low-density extrastriatal D2/D3 receptors, but it is uncertain whether [11C]FLB 457 can be used for measuring extrastriatal dopamine release.

Methods

We studied the effects of d-amphetamine (0.3 mg/kg i.v.) on extrastriatal [11C]FLB 457 binding potential (BPND) in a randomized, double-blind, placebo-controlled study including 24 healthy volunteers.

Results

The effects of d-amphetamine on [11C]FLB 457 BPND and distribution volume (VT) in the frontal cortex were not different from those of placebo. Small decreases in [11C]FLB 457 BPND were observed only in the posterior cingulate and hippocampus. The regional changes in [11C]FLB 457 BPND did not correlate with d-amphetamine-induced changes in subjective ratings of euphoria.

Conclusion

This placebo-controlled study showed that d-amphetamine does not induce marked changes in measures of extrastriatal dopamine D2/D3 receptor binding. Our results indicate that [11C]FLB 457 PET is not a useful method for measuring extrastriatal dopamine release in humans.