1373998-66-3Relevant academic research and scientific papers
Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent
Odan, Masahide,Ishizuka, Natsuki,Hiramatsu, Yoshiharu,Inagaki, Masanao,Hashizume, Hiroshi,Fujii, Yasuhiko,Mitsumori, Susumu,Morioka, Yasuhide,Soga, Masahiko,Deguchi, Masashi,Yasui, Kiyoshi,Arimura, Akinori
, p. 2898 - 2901 (2012/06/04)
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.
