TY - JOUR T1 - Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 1907 LP - 1912 DO - 10.2967/jnumed.118.211144 VL - 59 IS - 12 AU - Min-Jeong Kim AU - Stal S. Shrestha AU - Michelle Cortes AU - Prachi Singh AU - Cheryl Morse AU - Jeih-San Liow AU - Robert L. Gladding AU - Chad Brouwer AU - Katharine Henry AU - Evan Gallagher AU - George L. Tye AU - Sami S. Zoghbi AU - Masahiro Fujita AU - Victor W. Pike AU - Robert B. Innis Y1 - 2018/12/01 UR - http://jnm.snmjournals.org/content/59/12/1907.abstract N2 - This study assessed whether the newly developed PET radioligands 11C-PS13 and 11C-MC1 could image constitutive levels of cyclooxygenase (COX)-1 and COX-2, respectively, in rhesus monkeys. Methods: After intravenous injection of either radioligand, 24 whole-body PET scans were performed. To measure enzyme-specific uptake, scans of the 2 radioligands were also performed after administration of a nonradioactive drug preferential for either COX-1 or COX-2. Concurrent venous samples were obtained to measure parent radioligand concentrations. SUVs were calculated from 10 to 90 min. Results: 11C-PS13 showed specific uptake in most organs, including spleen, gastrointestinal tract, kidneys, and brain, which was blocked by COX-1, but not COX-2, preferential inhibitors. Specific uptake of 11C-MC1 was not observed in any organ except the ovaries and possibly kidneys. Conclusion: The findings suggest that 11C-PS13 has adequate signal in monkeys to justify its extension to human subjects. In contrast, 11C-MC1 is unlikely to show significant signal in healthy humans, though it may be able to do so in inflammatory conditions. ER -