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Radiosynthesis, In Vitro Validation, and In Vivo Evaluation of ¹⁸F-Labeled COX-1 and COX-2 Inhibitors

¹ Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri
² Discovery Research, Pharmacia Corporation, St. Louis, Missouri

View larger version (11K): [in a new window]   FIGURE 1. Structures of celecoxib (A) and rofecoxib (B).

View larger version (10K): [in a new window]   FIGURE 2. Structures of SC63217 (A) and SC58125 (B).

View larger version (13K): [in a new window]   FIGURE 3. Synthesis and radiosynthesis of 18F-SC58125 (compound 4a) and 18F-SC63217 (compound 4b).

View larger version (25K): [in a new window]   FIGURE 4. In vitro study on accumulation of 18F-SC58125 in J774 macrophage cells. Results are shown as mean ± SD (n = 3).

View larger version (29K): [in a new window]   FIGURE 5. In vitro study on accumulation of 18F-SC63217 in J774 macrophage cells. Results are shown as mean ± SD (n = 3).

View larger version (73K): [in a new window]   FIGURE 6. Sample PET images obtained from injection of 18F-SC58125 into mature female baboon. (A) Summed images over first 30 min after injection. (B) Summed images from 1 to 2 h after injection.