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Synthesis and In Vivo Evaluation of ¹⁸F-Desbromo-DuP-697 as a PET Tracer for Cyclooxygenase-2 Expression

PET Center, Groningen University Hospital, Groningen, The Netherlands

Cyclooxygenase-2 (COX-2) overexpression has been observed in various pathologies, such as inflammation, cancer, ischemia, and Alzheimer’s disease. As an initial step toward a noninvasive PET technique to assay COX-2 expression, this study describes the synthesis and preliminary evaluation of the radiolabeled COX-2 inhibitor ¹⁸F-desbromo-DuP-697. Methods: Desbromo-DuP-697 was radiolabeled by a nucleophilic aromatic substitution reaction of the nitro precursor with ¹⁸F-fluoride. Biodistribution studies of the tracer were performed in a carrageenan-induced hyperalgesia rat model. Brain uptake was investigated with autoradiography. To confirm the results of the biodistribution, COX activity was determined by a peroxidase assay. Results: Biodistribution studies showed specific binding of the tracer to COX-2 in heart, kidney, brain, and blood cells, but not in the inflamed paw, which was probably due to low COX-2 expression. In the brain, regional differences in tracer uptake were observed, with high uptake in cortical regions. ¹⁸F-Desbromo-DuP-697 did not show any binding to COX-1. Nonspecific uptake was high in fat and intestines. Conclusion: Because of its ability to cross the blood-brain barrier, ¹⁸F-desbromo-DuP-697 appears to be suitable for COX-2 imaging in the brain. Its high nonspecific uptake in the intestines may limit its use for imaging in the abdominal region.

Key Words: PET • desbromo-DuP-697 • cyclooxygenase-2 • inflammation • carrageenan

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