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      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.

      European Journal of Nuclear Medicine and Molecular Imaging

      Adult, Brain, drug effects, metabolism, radionuclide imaging, secretion, Carbon Radioisotopes, diagnostic use, Dextroamphetamine, pharmacology, Dopamine, Double-Blind Method, Frontal Lobe, Gyrus Cinguli, Hippocampus, Humans, Male, Positron-Emission Tomography, Pyrrolidines, Radiopharmaceuticals, Receptors, Dopamine D2, Receptors, Dopamine D3, Salicylamides, Young Adult

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          Abstract

          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. 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. 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. 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.

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          Journal
          18985345
          10.1007/s00259-008-0969-9

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