Automated radiosynthesis of [18F]PBR111 and [18F]PBR102 using the Tracerlab FXFN and Tracerlab MXFDG module for imaging the peripheral benzodiazepine receptor with PET

[18F]PBR111 and [18F]PBR102 are selective radioligands for imaging of the Peripheral Benzodiazepine Receptor (PBR). We have developed a fully automated method for the radiosynthesis of [18F]PBR111 and [18F]PBR102 in the Tracerlab FXFN (30±2% radiochemical yield non-decay-corrected for both tracers) and Tracerlab MXFDG (25±2% radiochemical yield non-decay-corrected for both tracers) from the corresponding p-toluenesulfonyl precursors. For all tracers, radiochemical purity was >99% and specific activity was >150 GBq/μmol after less than 60 min of preparation time.

► Radiosynthesis of novel ligands PBR111 and PBR102 with fluorine-18. ► Fully automated synthesis undertaken using the GE Tracerlab FXFN and MXFDG modules. ► Reproducible high yields suitable for clinical applications. ► Radiosynthesis and formulation achieved in less than 60 mins. ► PBR111 and PBR102 prepared in high radiochemical yield and specific activity.