Positron emission tomography imaging of (2R,3R)-5-[(18)F]fluoroethoxybenzovesamicol in rat and monkey brain: a radioligand for the vesicular acetylcholine transporter

Nucl Med Biol. 2009 Jul;36(5):489-93. doi: 10.1016/j.nucmedbio.2009.02.007. Epub 2009 May 8.


Introduction: The regional brain distribution of (2R,3R)-5-[(18)F]fluoroethoxy-benzovesamicol ((-)-[(18)F]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys.

Methods: Regional brain distributions of (-)-[(18)F]FEOBV in mice were determined using ex vivo dissection. MicroPET imaging was used to determine the regional brain pharmacokinetics of the radioligand in rat and rhesus monkey brains.

Results: In all three species, clear heterogeneous regional brain distributions were obtained, with the rank order of brain tissues (striatum>thalamus>cortex>cerebellum) consistent with the distribution of cholinergic nerve terminals containing the VAChT.

Conclusions: (-)-[(18)F]FEOBV remains a viable candidate for further development as an in vivo imaging agent for positron emission tomography (PET) studies of the VAChT in the human brain.

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Brain / metabolism*
  • Humans
  • Ligands
  • Macaca mulatta
  • Male
  • Mice
  • Piperidines / chemical synthesis
  • Piperidines / metabolism*
  • Piperidines / pharmacokinetics
  • Positron-Emission Tomography
  • Rats
  • Time Factors
  • Tissue Distribution
  • Vesicular Acetylcholine Transport Proteins / metabolism*


  • Ligands
  • Piperidines
  • Vesicular Acetylcholine Transport Proteins
  • fluoroethoxy-benzovesamicol