Improved Automated Radiosynthesis of [11C]PBR28

Kiran Kumar SOLINGAPURAM SAI; Don GAGE; Mike NADER; Robert H. MACH; Akiva MINTZ

doi:10.3797/scipharm.1505-06

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Article

19 June 2015

Improved Automated Radiosynthesis of [¹¹C]PBR28

and

Department of Radiology, Wake Forest School of Medicine, Medical Center Blvd, Winston-Salem, NC 27157, USA

Department of Physiology and Pharmacology, Wake Forest School of Medicine, Medical Center Blvd, Winston-Salem, NC 27157, USA

Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA

Author to whom correspondence should be addressed.

Sci. Pharm.2015, 83(3), 413-427;https://doi.org/10.3797/scipharm.1505-06

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Abstract

Microglial activation is commonly identified by elevated levels of the 18 kDa translocator protein (TSPO) in response to several inflammatory processes. [¹¹C]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 [¹¹C]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 [¹¹C]PBR28 had suitable kinetics with radiotracer accumulation observed in the caudate, putamen, cerebellum, and frontal cortex region.

Keywords:

Positron Emission Tomography (PET); Microglial activation; Synthesis; TSPO

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