PT  - JOURNAL ARTICLE
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
TI  - Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys
AID  - 10.2967/jnumed.118.211144
DP  - 2018 Dec 01
TA  - Journal of Nuclear Medicine
PG  - 1907--1912
VI  - 59
IP  - 12
4099  - http://jnm.snmjournals.org/content/59/12/1907.short
4100  - http://jnm.snmjournals.org/content/59/12/1907.full
SO  - J Nucl Med2018 Dec 01; 59
AB  - 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.