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PET imaging is a widely applicable but a very expensive technology. On-site synthesis is one important contributor to the high cost. In this report, we demonstrated the feasibility of a synthesis-free method for PET imaging of brown adipose tissue (BAT) and translocator protein 18 kDa (TSPO) via a combination of disulfiram, an FDA approved drug for alcoholism, and  64 CuCl 2  (termed  64 Cu-Dis). In this method, a step-wise injection protocol of  64 CuCl 2  and disulfiram was used to accomplish the purpose of synthesis-free. Specifically, disulfiram, an inactive  64 Cu ligand, was first injected to allow it to metabolize into diethyldithiocarbamate (DDC), a strong  64 Cu ligand, which can chelate  64 CuCl 2  from the following injection to form the actual PET tracer  in situ . Our blocking studies, western blot, and tissue histological imaging suggested that the observed BAT contrast was due to  64 Cu-Dis binding to TSPO, which was further confirmed as a specific biomarker for BAT imaging using [ 18 F]-F-DPA, a TSPO-specific PET tracer. Our studies, for the first time, demonstrated that TSPO could serve as a potential imaging biomarker for BAT. We believe that our strategy could be extended to other targets while significantly reducing the cost of PET imaging.

Synthesis-free PET imaging of brown adipose tissue and TSPO via combination of disulfiram and 64CuCl2