Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent |
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| Authors: | Odan Masahide Ishizuka Natsuki Hiramatsu Yoshiharu Inagaki Masanao Hashizume Hiroshi Fujii Yasuhiko Mitsumori Susumu Morioka Yasuhide Soga Masahiko Deguchi Masashi Yasui Kiyoshi Arimura Akinori |
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| Affiliation: | Shionogi Pharmaceutical Research Center, Shionogi & Co., Ltd, Toyonaka, Osaka, Japan. masahide.oodan@shionogi.co.jp |
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| Abstract: | The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid (21), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model. |
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