Preparation of the metabotropic glutamate receptor 5 (mGluR5) PET tracer [(18)F]FPEB for human use: An automated radiosynthesis and a novel one-pot synthesis of its radiolabeling precursor

Appl Radiat Isot. 2014 Dec:94:349-354. doi: 10.1016/j.apradiso.2014.09.006. Epub 2014 Sep 18.

Abstract

The radiotracer 3-[(18)F]fluoro-5-(2-pyridinylethynyl)benzonitrile, or [(18)F]FPEB, is a promising PET imaging agent for the metabotropic glutamate subtype 5 receptor (mGluR5). In an effort to develop a routine production method of this radiotracer for use in clinical research we adapted its radiosynthesis to an automated chemistry module. In the meanwhile, we also developed a simplified "one-pot" method for the preparation of the nitrobenzonitrile radiolabeling precursor for [(18)F]FPEB and its reference standard to replace the existing multi-step synthetic approach.

Keywords: PET; Radiotracer synthesis; Suzuki coupling; [(18)F]FPEB; mGluR5.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Fluorine Radioisotopes / chemistry*
  • Fluorine Radioisotopes / pharmacokinetics*
  • Humans
  • Isotope Labeling / methods*
  • Molecular Imaging / methods
  • Nitriles / chemical synthesis*
  • Nitriles / pharmacokinetics*
  • Positron-Emission Tomography / methods*
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacokinetics*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Receptor, Metabotropic Glutamate 5 / metabolism*
  • Robotics / methods

Substances

  • 3-fluoro-5-((pyridin-3-yl)ethynyl)benzonitrile
  • Fluorine Radioisotopes
  • Nitriles
  • Pyridines
  • Radiopharmaceuticals
  • Receptor, Metabotropic Glutamate 5