Abstract
This study assessed whether the newly developed PET radioligands11C-PS13 and11C-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 of11C-MC1 was not observed in any organ except the ovaries and possibly kidneys. Conclusion: The findings suggest that11C-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.
Original language | English (US) |
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Pages (from-to) | 1907-1912 |
Number of pages | 6 |
Journal | Journal of Nuclear Medicine |
Volume | 59 |
Issue number | 12 |
DOIs | |
State | Published - Dec 1 2018 |
Keywords
- Cyclooxygenase-1
- Cyclooxygenase-2
- Inflammation
- Nonsteroidal antiinflammatory agents
- Positron-emission tomography
ASJC Scopus subject areas
- Radiology Nuclear Medicine and imaging