Discovery of S-777469: An orally available CB2 agonist as an antipruritic agent

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• 作者：Masahide Odan ; ^{masahide.oodan@shionogi.co.jp} ; Natsuki Ishizuka ; Yoshiharu Hiramatsu ; Masanao Inagaki ; Hiroshi Hashizume ; Yasuhiko Fujii ; Susumu Mitsumori ; Yasuhide Morioka ; Masahiko Soga ; Masashi Deguchi ; Kiyoshi Yasui ; Akinori Arimura
• 关键词：Cannabinoid ; CB receptor agonist ; GPCR ; Antipruritics
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April, 2012
• 卷：22
• 期：8
• 页码：2803-2806
• 文件大小：1265 K

摘要

The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure-activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55%and 61%, respectively).