期刊
JOURNAL OF NUCLEAR MEDICINE
卷 59, 期 12, 页码 1907-1912出版社
SOC NUCLEAR MEDICINE INC
DOI: 10.2967/jnumed.118.211144
关键词
cyclooxygenase-1; cyclooxygenase-2; positron-emission tomography; inflammation; nonsteroidal antiinflammatory agents
资金
- Intramural Research Program of the National Institute of Mental Health, National Institutes of Health [ZIAMH002795, ZIAMH002793]
- NATIONAL INSTITUTE OF MENTAL HEALTH [ZIAMH002795, ZIAMH002793, ZIAMH002852] Funding Source: NIH RePORTER
This study assessed whether the newly developed PET radioligands C-11-PS13 and C-11-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: C-11-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 C-11-MC1 was not observed in any organ except the ovaries and possibly kidneys. Conclusion: The findings suggest that C-11-PS13 has adequate signal in monkeys to justify its extension to human subjects. In contrast, C-11-MC1 is unlikely to show significant signal in healthy humans, though it may be able to do so in inflammatory conditions.
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