Details

Autor(en) / Beteiligte

• 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

Titel

Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys

Ist Teil von

• Journal of Nuclear Medicine, 2018-12, Vol.59 (12), p.1907-1912

Ort / Verlag

United States: Society of Nuclear Medicine

Erscheinungsjahr

2018

Link zum Volltext

Quelle

Elektronische Zeitschriftenbibliothek

Beschreibungen/Notizen

• This study assessed whether the newly developed PET radioligands C-PS13 and C-MC1 could image constitutive levels of cyclooxygenase (COX)-1 and COX-2, respectively, in rhesus monkeys. 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. C-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-MC1 was not observed in any organ except the ovaries and possibly kidneys. The findings suggest that C-PS13 has adequate signal in monkeys to justify its extension to human subjects. In contrast, C-MC1 is unlikely to show significant signal in healthy humans, though it may be able to do so in inflammatory conditions.