title: Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
abstract: 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).
authors.affiliation: Shionogi Pharmaceutical Research Center, Shionogi & Co., Ltd 1-1, Toyonaka, Osaka, Japan. masahide.oodan@shionogi.co.jp
authors.forename: Masahide
authors.initials: M
authors.lastname: Odan
authors.forename: Natsuki
authors.initials: N
authors.lastname: Ishizuka
authors.forename: Yoshiharu
authors.initials: Y
authors.lastname: Hiramatsu
authors.forename: Masanao
authors.initials: M
authors.lastname: Inagaki
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Hashizume
authors.forename: Yasuhiko
authors.initials: Y
authors.lastname: Fujii
authors.forename: Susumu
authors.initials: S
authors.lastname: Mitsumori
authors.forename: Yasuhide
authors.initials: Y
authors.lastname: Morioka
authors.forename: Masahiko
authors.initials: M
authors.lastname: Soga
authors.forename: Masashi
authors.initials: M
authors.lastname: Deguchi
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Yasui
authors.forename: Akinori
authors.initials: A
authors.lastname: Arimura
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000982:Antipruritics / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D004195:Disease Models, Animal; D020128:Inhibitory Concentration 50; D008024:Ligands; D051379:Mice; D008813:Mice, Inbred ICR; D015394:Molecular Structure; D011485:Protein Binding / Q000187:drug effects; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*
chemical_list: D000982:Antipruritics; D008024:Ligands; D011728:Pyridones; D043885:Receptor, Cannabinoid, CB2; C574957:S-777469