2. Academic Validation
  3. Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent

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

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2803-6. doi: 10.1016/j.bmcl.2012.02.072.
Masahide Odan 1,  Natsuki Ishizuka,  Yoshiharu Hiramatsu,  Masanao Inagaki,  Hiroshi Hashizume,  Yasuhiko Fujii,  Susumu Mitsumori,  Yasuhide Morioka,  Masahiko Soga,  Masashi Deguchi,  Kiyoshi Yasui,  Akinori Arimura
Affiliations

Affiliation

  • 1 Shionogi Pharmaceutical Research Center, Shionogi & Co., Ltd 1-1, Toyonaka, Osaka, Japan. [email protected]
PMID: 22444677 DOI: 10.1016/j.bmcl.2012.02.072
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).

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