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.
Highlights
Expression of the peripheral benzodiazepine receptors (PBR), recently described as the 18 kDa translocator protein TSPO, is considered to be a hallmark for microglial activation [1, 2]
Solingapuram Sai et al.: transportation, immune alterations, and apoptosis are associated with the transmembrane channels of the mitochondrial membrane, which are considered as a depository for TSPO [1, 6,7,8,9,10]
Imaging microglial activation by targeting TSPO may provide an efficient index of the disease progression, and enhance the therapeutic planning for diseases affected by neuroinflammatory processes [15]
Summary
Expression of the peripheral benzodiazepine receptors (PBR), recently described as the 18 kDa translocator protein TSPO, is considered to be a hallmark for microglial activation [1, 2]. The radiochemical synthesis of [11C]PBR28 was carried out by alkylating the corresponding p-phenol precursor 6 with [11C]MeI in DMSO using NaOH as depicted in Scheme 2.
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