Synthesis, radiolabeling and initial in vivo evaluation of [11 C] KSM-01 for imaging PPAR-α receptors

…, JM Rothfuss, KI Shoghi, MJ Welch, RJ Gropler…

文献索引：Solingapuram Sai, Kiran Kumar; Kil, Kun-Eek; Tu, Zhude; Chu, Wenhua; Finck, Brian N.; Rothfuss, Justin M.; Shoghi, Kooresh I.; Welch, Michael J.; Gropler, Robert J.; Mach, Robert H. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6233 - 6236

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被引用次数: 3

摘要

Peroxisome proliferator-activated receptor alpha (PPAR-α) is a ligand-activated nuclear receptor transcription factor that regulates the fatty acid β-oxidation. An in vitro assay identified the p-methoxy phenyl ureido thiobutyric acid derivative KSM-01 (IC50= 0.28±0.09 nM) having a higher affinity to activate PPAR-α than the PPAR-α agonist GW7647 (IC50= 0.46±0.19 nM). In this study, we report the synthesis and initial in vivo evaluation of [11C] ...