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Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys.
Kim, Min-Jeong; Shrestha, Stal S; Cortes, Michelle; Singh, Prachi; Morse, Cheryl; Liow, Jeih-San; Gladding, Robert L; Brouwer, Chad; Henry, Katharine; Gallagher, Evan; Tye, George L; Zoghbi, Sami S; Fujita, Masahiro; Pike, Victor W; Innis, Robert B.
Afiliación
  • Kim MJ; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland min-jeong.kim@nih.gov.
  • Shrestha SS; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Cortes M; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Singh P; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Morse C; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Liow JS; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Gladding RL; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Brouwer C; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Henry K; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Gallagher E; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Tye GL; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Zoghbi SS; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Fujita M; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Pike VW; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
  • Innis RB; Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland.
J Nucl Med ; 59(12): 1907-1912, 2018 12.
Article en En | MEDLINE | ID: mdl-29959215
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Radiofármacos / Tomografía de Emisión de Positrones / Ciclooxigenasa 1 / Ciclooxigenasa 2 Límite: Animals Idioma: En Revista: J Nucl Med Año: 2018 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Radiofármacos / Tomografía de Emisión de Positrones / Ciclooxigenasa 1 / Ciclooxigenasa 2 Límite: Animals Idioma: En Revista: J Nucl Med Año: 2018 Tipo del documento: Article Pais de publicación: Estados Unidos