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A PET study of

Lars Farde, Nathalie Ginovart, Christer Halldin

    The International Journal of Neuropsychopharmacology
    |May 10, 2001
    PubMed
    Summary
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    [11C]ß-CIT-FE is a promising radioligand for imaging the dopamine transporter using positron emission tomography (PET). This tracer shows high specific binding in primate and human brains, making it suitable for neuropsychiatric and drug abuse research.

    Area of Science:

    • Neuroscience
    • Radiochemistry
    • Nuclear Medicine

    Background:

    • Radiolabeled cocaine analogues are explored for brain dopamine transporter imaging in neuropsychiatric disorders and drug abuse.
    • Previous studies demonstrated high specific binding of [11C]ß-CIT-FE in monkey striatum using positron emission tomography (PET).

    Purpose of the Study:

    • To evaluate the selectivity and suitability of [11C]ß-CIT-FE as a radioligand for dopamine transporter imaging in the primate and human brain.
    • To assess the binding characteristics and quantitative potential of [11C]ß-CIT-FE for clinical applications.

    Main Methods:

    • Primate brain studies involved pretreatment with reference ligands for dopamine, serotonin, and norepinephrine transporters to assess selectivity.
    • Human studies in three healthy subjects analyzed regional binding using equilibrium and kinetic analyses, including Scatchard analysis.

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  • Pharmacological characterization and quantitative approaches like binding potential estimation were employed.

    • Main Results:

    • [11C]ß-CIT-FE demonstrated saturable binding in the primate striatum, consistent with dopamine transporter density.
    • Pharmacological data confirmed that striatal binding primarily represents the dopamine transporter.
    • In human subjects, the radioligand showed high brain uptake, reaching peak equilibrium within 1 hour post-injection.
    • Various quantitative methods yielded consistent binding potential values.

    Conclusions:

    • [11C]ß-CIT-FE is a selective and effective radioligand for imaging the dopamine transporter in the brain.
    • Its favorable uptake kinetics and binding characteristics make it suitable for clinical PET studies, especially those requiring short acquisition times or repeated measures.