Improved Automated Radiosynthesis of [(11)C]PBR28.

Sci Pharm

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

Published: February 2016

AI Article Synopsis

  • Microglial activation can be detected by monitoring the 18 kDa translocator protein (TSPO), which increases during inflammatory processes.
  • The PET tracer [(11)C]PBR28 shows promise for imaging TSPO in humans and primates, with improvements made in its radiolabeling process for better efficiency.
  • Dynamic PET imaging of rhesus monkeys revealed good distribution of [(11)C]PBR28 in key brain regions, indicating its potential for studying brain inflammation.

Article 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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4727796PMC
http://dx.doi.org/10.3797/scipharm.1505-06DOI Listing

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