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In Vivo Imaging of Vesicular Monoamine Transporters in Human Brain Using [11C]Tetrabenazine and Positron Emission Tomography

Authors

  • Michael R. Kilbourn,

    Corresponding author
    1. Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor, Michigan, U.S.A.
      Address correspondence and reprint requests to Dr. M. R. Kilbourn at 3480 Kresge III, University of Michigan, Ann Arbor, MI 49109–0552, U.S.A.
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  • Jean N. DaSilva,

    1. Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor, Michigan, U.S.A.
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  • Kirk A. Frey,

    1. Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor, Michigan, U.S.A.
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  • Robert A. Koeppe,

    1. Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor, Michigan, U.S.A.
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  • David E. Kuhl

    1. Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor, Michigan, U.S.A.
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Address correspondence and reprint requests to Dr. M. R. Kilbourn at 3480 Kresge III, University of Michigan, Ann Arbor, MI 49109–0552, U.S.A.

Abstract

Abstract: The pharmacokinetics of [11CJtetrabenazine, a high-affinity radioligand for the monoamine vesicular transporter, were determined in living human brain using in vivo imaging by positron emission tomography (PET). The radiotracer showed high brain uptake and rapid washout from all brain regions with relatively slower clearance from regions of highest concentrations of monoamine vesicular transporters (striatum), resulting in clear differential visualization of these structures at short intervals after injection (10–20 min). As the first human PET imaging study of a vesicular neurotransmitter transporter, these experiments demonstrate that external imaging of vesicular transporters forms a new and valuable approach to the in vivo quantification of monoaminergic neurons, with potential application to the in vivo study of neurodegenerative disorders such as Parkinson's disease.

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