Biodistribution and radiation dosimetry of the norepinephrine transporter radioligand (S,S)-[18F]FMeNER-D2: a human whole-body PET study

Eur J Nucl Med Mol Imaging. 2008 Mar;35(3):630-6. doi: 10.1007/s00259-007-0622-z. Epub 2007 Nov 14.

Abstract

Purpose: (S,S)-[(18)F]FMeNER-D(2) is a recently developed positron-emission tomography (PET) radioligand for in vivo quantification of the norepinephrine transporter system. The aim of this study was to provide dosimetry estimates for (S,S)-[(18)F]FMeNER-D(2) based on human whole-body PET measurements.

Methods: PET scans were performed for a total of 6.4 h after the injection of 168.9 +/- 31.5 MBq of (S,S)-[(18)F]FMeNER-D(2) in four healthy male subjects. Volumes of interest were drawn on the coronal images. Estimates of the absorbed dose of radiation were calculated using the OLINDA software.

Results: Uptake was largest in lungs, followed by liver, bladder, brain and other organs. Peak values of the percent injected dose (%ID) at a time after radioligand injection were calculated for the lung (21.6%ID at 0.3 h), liver (5.1%ID at 0.3 h), bladder (12.2%ID at 6 h) and brain (2.3%ID at 0.3 h). The largest absorbed dose was found in the urinary bladder wall (0.039 mGy/MBq). The calculated effective dose was 0.017 mSv/MBq.

Conclusion: Based on the distribution and dose estimates, the estimated radiation burden of (S,S)-[(18)F]FMeNER-D(2) is lower than that of [(18)F]FDG. The radioligand would allow multiple PET examinations in the same research subject per year.

MeSH terms

  • Body Burden
  • Humans
  • Ligands
  • Metabolic Clearance Rate
  • Morpholines / analysis*
  • Morpholines / pharmacokinetics*
  • Norepinephrine Plasma Membrane Transport Proteins / metabolism*
  • Organ Specificity
  • Positron-Emission Tomography / methods
  • Radiation Dosage
  • Radiometry*
  • Relative Biological Effectiveness
  • Tissue Distribution
  • Whole Body Imaging / methods*

Substances

  • 2-(alpha-(2-fluoromethoxyphenoxy)benzyl)morpholine
  • Ligands
  • Morpholines
  • Norepinephrine Plasma Membrane Transport Proteins