RT Journal Article
SR Electronic
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
FD Society of Nuclear Medicine
SP 1907
OP 1912
DO 10.2967/jnumed.118.211144
VO 59
IS 12
A1 Min-Jeong Kim
A1 Stal S. Shrestha
A1 Michelle Cortes
A1 Prachi Singh
A1 Cheryl Morse
A1 Jeih-San Liow
A1 Robert L. Gladding
A1 Chad Brouwer
A1 Katharine Henry
A1 Evan Gallagher
A1 George L. Tye
A1 Sami S. Zoghbi
A1 Masahiro Fujita
A1 Victor W. Pike
A1 Robert B. Innis
YR 2018
UL http://jnm.snmjournals.org/content/59/12/1907.abstract
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.