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Synthesis and Biodistribution of ¹¹C-GW7845, a Positron-Emitting Agonist for Peroxisome Proliferator–Activated Receptor-

¹ Department of Radiology, Johns Hopkins University, Baltimore, Maryland
² Guilford Pharmaceuticals, Baltimore, Maryland
³ Research and Development, GlaxoSmithKline, Research Triangle Park, North Carolina

View larger version (19K): [in a new window]   FIGURE 1. Synthesis of 11C-compound 1. OMe = methoxy (OCH3); Ki = inhibitor constant.

View larger version (12K): [in a new window]   FIGURE 2. Binding selectivity of 11C-compound 1 at 60 min after injection (n = 3) in female SCID mice bearing MCF-7 tumors. Tissue distribution of 11C-compound 1 upon coinjection with unlabeled compound 1 at 2 mg/kg showed either equal or increased tracer uptake. Error bars indicate SDs.

View larger version (34K): [in a new window]   FIGURE 3. (A) PET image showing in vivo distribution of 11C-compound 1 at 60 min after injection in SCID mice bearing MDA-MB-231 tumors. Tissue distribution of 11C-compound 1 after intraperitoneal administration of unlabeled compound 1 at 2 mg/kg showed either equal or increased tracer uptake. (B) CT image of same mice.