Pharmacokinetics and dosimetry of iodine-123 labelled PE2I in humans, a radioligand for dopamine transporter imaging

Jyrki T. Kuikka, Jean L. Baulieu, Jukka Hiltunen, Christer Halldin, Kim A. Bergström, Lars Farde, Patrik Emond, Sylvie Chalon, Meixiang Yu, Tuomo Nikula, Tomi Laitinen, Jari Karhu, Erkki Tupala, Tero Hallikainen, Ville Kolehmainen, Laurent Mauclaire, Bernard Maziere, Jari Tiihonen, Denis Guilloteau

Research output: Contribution to journalArticle

47 Scopus citations

Abstract

The iodine-123 labelled selective ligand N-(3-iodoprop-2E-enyl)-2-β-carbomethoxy-3β-(4-methylphenyl)nortropane ([123I]PE2I) was evaluated as a probe for in vivo dopamine transporter imaging in the human brain, Six healthy subjects were imaged with a high-resolution single-photon emission tomography scanner. Striatal radioactivity peaked at 1 h after injection. The background radioactivity was low. The volume of distribution in the striatum was 94 ± 24 ml/ml. The results were compared with those of [123I]β-CIT imaging. There was no significant uptake of [123I]PE2I in serotonin-rich regions such as the midbrain, hypothalamus and anterior gingulus, suggesting that in vivo binding is specific for the dopamine transporter. One main polar metabolite of [123I]PE2I was found in plasma, and the parent plasma concentration decayed rapidly. Radiation exposure to the study subject is 0.022 ± 0.004 mSv/MBq (effective dose). The preliminary results suggest that [123I]PE2I is a selective SPET ligand for imaging striatal dopamine transporter density.

Original languageEnglish (US)
Pages (from-to)531-534
Number of pages4
JournalEuropean Journal of Nuclear Medicine
Volume25
Issue number5
DOIs
StatePublished - Jan 1 1998

Keywords

  • Dopamine transporter
  • Human brain
  • Single-photon emission tomography
  • Striatum

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

Fingerprint Dive into the research topics of 'Pharmacokinetics and dosimetry of iodine-123 labelled PE2I in humans, a radioligand for dopamine transporter imaging'. Together they form a unique fingerprint.

Cite this