Evaluation of two potent and selective PET radioligands to image COX-1 and COX-2 in rhesus monkeys

Min Jeong Kim, Stal S. Shrestha, Michelle Cortes, Prachi Singh, Cheryl Morse, Jeih San Liow, Robert L. Gladding, Chad Brouwer, Katharine Henry, Evan Gallagher, George L. Tye, Sami S. Zoghbi, Masahiro Fujita, Victor W. Pike, Robert B. Innis

Research output: Contribution to journalArticle

14 Scopus citations

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 languageEnglish (US)
Pages (from-to)1907-1912
Number of pages6
JournalJournal of Nuclear Medicine
Volume59
Issue number12
DOIs
StatePublished - Dec 1 2018

Keywords

  • Cyclooxygenase-1
  • Cyclooxygenase-2
  • Inflammation
  • Nonsteroidal antiinflammatory agents
  • Positron-emission tomography

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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