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First Evaluation in Humans of [123I]PE2I: A Selective Radioligand for Visualization of the Striatal Dopamine Transporter Density

  • K. A. Bergström
  • J. T. Kuikka
  • P. Emond
  • J. Hiltunen
  • C. Halldin
  • D. Guilloteau
  • L. Mauclaire
  • M. Yu
  • J. Karhu
  • E. Tupala
  • J. Tiihonen
Conference paper
Part of the Advances in Pharmacological Sciences book series (APS)

Abstract

(E)-N-(3-iodoprop-2-enyl)-2β-Carbomethoxy-3β-(4-methylphenyl)nortropane (PE2I) is recently synthesised selective compound for the dopamine transporter. In the present study 123I-labelled PE2I were prepared for SPET studies with healthy volunteers. There was a rapid uptake of radioactivity in brain (3% of ID at 1 hour) and a high accumulation of radioactivity in the striatum. In the thalamus and in cortical regions no visible uptake of radioactivity was observed. Striatum-to-cerebellum ratio was 5 at 70 min. Percentage of unchanged [123I]PE2I in plasma was less than 20% at 1 h post injection. In conclusion, [123I]PE2I is a potential radioligand for the dopamine transporter imaging with SPET.

Keywords

Positron Emission Tomography Dopamine Transporter Gradient HPLC Selective Compound SPET Study 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer Basel AG 1999

Authors and Affiliations

  • K. A. Bergström
    • 1
  • J. T. Kuikka
    • 1
  • P. Emond
    • 2
  • J. Hiltunen
    • 3
  • C. Halldin
    • 4
  • D. Guilloteau
    • 2
  • L. Mauclaire
    • 5
  • M. Yu
    • 1
  • J. Karhu
    • 1
  • E. Tupala
    • 6
  • J. Tiihonen
    • 6
  1. 1.Department of Clinical PhysiologyKuopio University HospitalKuopioFinland
  2. 2.Laboratoire de Biophysique Médicale et PharmaceutiqueUniversité François RabelaisToursFrance
  3. 3.MAP Medical Technologies Inc.TikkakoskiFinland
  4. 4.Department of Clinical Neuroscience, Psychiatry SectionKarolinska InstituteStockholmSweden
  5. 5.CIS-Bio industrieGif-sur-YvetteFrance
  6. 6.Department of Forensic PsychiatryUniversity of Kuopio, Niuvanniemi HospitalKuopioFinland

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