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.

Author(s): Aalto S, Hirvonen J, Kaasinen V, Hagelberg N, Kajander J, Nagren K, Seppala T, Rinne JO, Scheinin H, Hietala J

Affiliation(s): Turku PET Centre, University of Turku, 20014 Turku, Finland.

Publication date & source: 2009-03, Eur J Nucl Med Mol Imaging., 36(3):475-83. Epub 2008 Nov 5.

Publication type: Randomized Controlled Trial; Research Support, Non-U.S. Gov't

PURPOSE: The dopamine D(2)/D(3) receptor ligand [(11)C]FLB 457 and PET enable quantification of low-density extrastriatal D(2)/D(3) receptors, but it is uncertain whether [(11)C]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 [(11)C]FLB 457 binding potential (BP(ND)) in a randomized, double-blind, placebo-controlled study including 24 healthy volunteers. RESULTS: The effects of d-amphetamine on [(11)C]FLB 457 BP(ND) and distribution volume (V(T)) in the frontal cortex were not different from those of placebo. Small decreases in [(11)C]FLB 457 BP(ND) were observed only in the posterior cingulate and hippocampus. The regional changes in [(11)C]FLB 457 BP(ND) 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 D(2)/D(3) receptor binding. Our results indicate that [(11)C]FLB 457 PET is not a useful method for measuring extrastriatal dopamine release in humans.