Dopamine transporter imaging with fluorine-18-FPCIT and PET

Ken Kazumata, Vijay Dhawan, Thomas Chaly, Angelo Antonini, Claude Margouleff, Abdelfatihe Belakhlef, John Neumeyer, David Eidelberg

Research output: Contribution to journalArticle

Abstract

Fluorinated N-3-fluoropropyl-2-β-carboxymethoxy-3-β-(4-iodophenyl) nortropane (FPCIT) has been synthesized as a dopamine transporter ligand for PET studies. We evaluated the regional brain uptake and the plasma metabolism of [18F]-FPCIT. Methods: PET studies were conducted on 7 normal subjects and on 10 patients with Parkinson's disease. After the [18F]-FPCIT injection (4.4 ± 1.8 mCi), dynamic scans were acquired over 100 min. Plasma metabolite analysis was performed using high-performance liquid chromatography (HPLC). Results: Plasma HPLC revealed two peaks corresponding to unmetabolized [18F]-FPCIT and a polar metabolite. The fraction of the parent compound decreased rapidly to 25% at 25 min. Fluorine-18-FPCIT showed a striatum-to-occipital ratio (SOR) of 3.5 at 90 min postinjection. The ratio of striatal-to-occipital distribution volume (DVR) was calculated directly by using a mean tissue-to-plasma efflux constant for occipital cortex obtained in 10 subjects (k2/' = 0.037 min-1). DVR measures determined with and without plasma input function were correlated (r = 0.98, p <0.0001). In normal subjects, a significant age-related decline of DVR was observed both for caudate and putamen, corresponding to a 7.7% and 6.4% decline per decade, respectively (r > 0.85, p <0.01). Both DVR and SOR correctly classified early-stage Parkinson's disease patients with comparable accuracy (p <0.0001). Age-corrected DVR values correlated negatively with the Uniform Parkinson's Disease Rating Scale composite motor ratings (r = 0.66, p <0.05). Conclusion: The tracer characteristics are compatible with a high- affinity, reversible ligand. FPCIT/PET demonstrated age-related decline in dopamine transporter binding in normal subjects as well as significant reductions in patients with idiopathic Parkinson's disease, which correlates with the disease severity.

Original languageEnglish
Pages (from-to)1521-1530
Number of pages10
JournalJournal of Nuclear Medicine
Volume39
Issue number9
Publication statusPublished - Sep 1998

Keywords

  • Aging effect
  • Dopamine transporters
  • Fluorine-18-fluorinated N-3-fluoropropyl-2-β-carboxymethoxy-3-β-(4- iodophenyl) nortropane
  • Parkinson's disease
  • PET

ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

Fingerprint Dive into the research topics of 'Dopamine transporter imaging with fluorine-18-FPCIT and PET'. Together they form a unique fingerprint.

  • Cite this

    Kazumata, K., Dhawan, V., Chaly, T., Antonini, A., Margouleff, C., Belakhlef, A., Neumeyer, J., & Eidelberg, D. (1998). Dopamine transporter imaging with fluorine-18-FPCIT and PET. Journal of Nuclear Medicine, 39(9), 1521-1530.