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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

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European Journal of Nuclear Medicine and Molecular Imaging Aims and scope Submit manuscript

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.

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Acknowledgements

The technical assistance of the staff of Turku PET centre is gratefully acknowledged. We thank Aino Kankaanpää (National Public Health Institute) for the measurement of d-amphetamine concentrations in plasma. This study was supported financially by clinical grants (EVO) from Turku University Hospital, and by the Academy of Finland (project nos. 111879 and 210825).

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Authors and Affiliations

  1. Turku PET Centre, University of Turku, 20014, Turku, Finland

    Sargo Aalto, Jussi Hirvonen, Nora Hagelberg, Jaana Kajander, Kjell Någren, Juha O. Rinne, Harry Scheinin & Jarmo Hietala

  2. Department of Psychology, Åbo Akademi University, Nunnegatan 4, 20500, Turku, Finland

    Sargo Aalto

  3. Department of Neurology, University of Turku, P.O. Box 52, 20521, Turku, Finland

    Valtteri Kaasinen

  4. Department of Anaesthesiology, Intensive Care, Emergency Care and Pain Medicine, Turku University Central Hospital, Turku, Finland

    Nora Hagelberg

  5. National Public Health Institute, Drug Research Unit, Helsinki, Finland

    Timo Seppälä

  6. Department of Pharmacology, Drug Development and Therapeutics, University of Turku, Kiinamyllynkatu 10, 20520, Turku, Finland

    Harry Scheinin

  7. Department of Psychiatry, University of Turku, Kunnallissairaalantie 20, Building 9, 20700, Turku, Finland

    Jarmo Hietala

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  1. Sargo Aalto
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Correspondence to Jarmo Hietala.

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Aalto, S., Hirvonen, J., Kaasinen, V. et al. 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. Eur J Nucl Med Mol Imaging 36, 475–483 (2009). https://doi.org/10.1007/s00259-008-0969-9

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  • DOI: https://doi.org/10.1007/s00259-008-0969-9

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