Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor

Bioorg Med Chem Lett. 2014 Jan 1;24(1):283-7. doi: 10.1016/j.bmcl.2013.11.023. Epub 2013 Nov 20.

Abstract

Cannabinoid CB2 PET tracers are considered as a promising alternative to PBR/TSPO tracers for the in-vivo imaging of neuroinflammation. We describe here the synthesis and characterization of compound 3, a new potent and brain penetrating CB2 ligand based on an original triazine template. The PET tracer [(18)F]-dideutero-3 was prepared in a three steps radiosynthesis, and demonstrated significant uptake in rhesus macaque and baboon brain with a maximum SUV of about 0.7-0.9g/mL, followed by a moderate washout over time.

Keywords: CB2; Cannabinoid; Imaging; PET; Triazine.

MeSH terms

  • Animals
  • Brain / metabolism
  • Fluorine Radioisotopes / chemistry
  • Fluorine Radioisotopes / metabolism*
  • Fluorine Radioisotopes / pharmacokinetics
  • Humans
  • Ligands
  • Macaca mulatta
  • Molecular Structure
  • Papio
  • Positron-Emission Tomography*
  • Receptor, Cannabinoid, CB2 / metabolism*
  • Triazines / chemical synthesis
  • Triazines / metabolism*
  • Triazines / pharmacokinetics

Substances

  • Fluorine Radioisotopes
  • Ligands
  • Receptor, Cannabinoid, CB2
  • Triazines