Preparation of the Metabotropic Glutamate Receptor 5 (mGluR5) PET Tracer 18FFPEB for Human Use: An Automated Radiosynthesis and a Novel One-Pot Synthesis of its Radiolabeling Precursor

摘要

The radiotracer 3-[¹⁸F]fluoro-5-(2-pyridinylethynyl)benzonitrile, or [¹⁸F]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 [¹⁸F]FPEB and its reference standard to replace the existing multi-step synthetic approach.