Simplified quantification and whole-body distribution of [18F]FE-PE2I in nonhuman primates: prediction for human studies

Nucl Med Biol. 2012 Feb;39(2):295-303. doi: 10.1016/j.nucmedbio.2011.08.004. Epub 2011 Oct 26.

Abstract

Introduction: [(18)F]FE-PE2I is a promising dopamine transporter (DAT) radioligand. In nonhuman primates, we examined the accuracy of simplified quantification methods and the estimates of radiation dose of [(18)F]FE-PE2I.

Methods: In the quantification study, binding potential (BP(ND)) values previously reported in three rhesus monkeys using kinetic and graphical analyses of [(18)F]FE-PE2I were used for comparison. BP(ND) using the cerebellum as reference region was obtained with four reference tissue methods applied to the [(18)F]FE-PE2I data that were compared with the kinetic and graphical analyses. In the whole-body study, estimates of adsorbed radiation were obtained in two cynomolgus monkeys.

Results: All reference tissue methods provided BP(ND) values within 5% of the values obtained with the kinetic and graphical analyses. The shortest imaging time for stable BP(ND) estimation was 54 min. The average effective dose of [(18)F]FE-PE2I was 0.021 mSv/MBq, similar to 2-deoxy-2-[(18)F]fluoro-d-glucose.

Conclusions: The results in nonhuman primates suggest that [(18)F]FE-PE2I is suitable for accurate and stable DAT quantification, and its radiation dose estimates would allow for a maximal administered radioactivity of 476 MBq in human subjects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dopamine Plasma Membrane Transport Proteins / metabolism
  • Female
  • Fluorine Radioisotopes / pharmacokinetics*
  • Macaca fascicularis
  • Macaca mulatta
  • Nortropanes / pharmacokinetics*
  • Positron-Emission Tomography / methods*
  • Radiation Dosage*
  • Tissue Distribution
  • Whole Body Imaging / methods*

Substances

  • (E)-N-(3-iodoprop-2-enyl)-2beta-carbofluoroethoxy-3beta-(4'-methyl-phenyl) nortropane
  • Dopamine Plasma Membrane Transport Proteins
  • Fluorine Radioisotopes
  • Nortropanes