Improved Automated Radiosynthesis of [(11)C]PBR28

Sci Pharm. 2015 Jun 19;83(3):413-27. doi: 10.3797/scipharm.1505-06. Print 2015 Jul-Sep.

Abstract

Microglial activation is commonly identified by elevated levels of the 18 kDa translocator protein (TSPO) in response to several inflammatory processes. [(11)C]PBR28 is one of the most promising PET tracers to image TSPO in both human and non-human primates. In this study, we optimized the radiolabeling procedure of [(11)C]PBR28 for higher radiochemical yield, radiochemical purity, and specific activity, which can be easily translated to any automated module for clinical trials. Time-activity curves (TACs) derived from the dynamic PET imaging of male rhesus monkey brains demonstrated that [(11)C]PBR28 had suitable kinetics with radiotracer accumulation observed in the caudate, putamen, cerebellum, and frontal cortex region.

Keywords: Microglial activation; Positron Emission Tomography (PET); Synthesis; TSPO.