Synthesis of 3H, 13C2, 2H414C‐SCH 430765 and 35S‐SCH 500946, potent and selective inhibitors of the NPY5 receptor

Hesk, D., Koharski, D., Mcnamara, P., Royster, P., Saluja, S., Truong, V., & Voronin, K. (2018). Synthesis of 3H, 13C2, 2H414C‐SCH 430765 and 35S‐SCH 500946, potent and selective inhibitors of the NPY5 receptor. Journal of Labelled Compounds and Radiopharmaceuticals, 61(7), 533-539. https://doi.org/10.1002/jlcr.v61.7

Abstract

SCH 430765 and SCH 500496 are potent and selective antagonists of the NPY5 receptor. NPY5 receptor antagonists have the potential for the treatment of obesity. [35S]SCH 500946 was prepared for a competition binding assay which led to the identification of SCH 430765. Three distinct isotopically labelled forms of SCH 430765 were synthesized. [3H]SCH 430765 was prepared for a preliminary absorption, distribution, metabolism and excretion data evaluation of the compound and [14C]SCH 430765 for more definitive absorption, distribution, metabolism and excretion data work. In addition, [13C2,2H4]SCH 430765 was prepared as an internal standard for a LC‐MS bioanalytical method. The paper discusses the synthesis of 3 isotopically labelled forms of SCH 430765 and [35S]SCH 500946.

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