Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation

…, W Thomsen, K Whelan, D Sengupta, M Morgan…

文献索引：Semple, Graeme; Tran, Thuy-Anh; Kramer, Bryan; Hsu, Debbie; Han, Sangdon; Choi, Juyi; Vallar, Pureza; Casper, Martin D.; Zou, Ning; Hauser, Erin K.; Thomsen, William; Whelan, Kevin; Sengupta, Dipanjan; Morgan, Michael; Sekiguchi, Yoshinori; Kanuma, Kosuke; Chaki, Shigeyuki; Grottick, Andrew J. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 21 p. 6166 - 6171

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被引用次数: 4

摘要

A series of pyrimidine analogues derived from ATC0175 were potent antagonists of human MCH-R1 in vitro. Significantly improved receptor selectivity was achieved with several analogues from this series, but no improvement in brain partitioning was noted. One example from this series was shown to inhibit food intake and decrease body weight in a chronic study. However no clear correlation between the pharmacodynamic effect and the ...