S-777,469 Explained
S-777,469 is a drug developed by Shionogi which is a cannabinoid receptor agonist, with 128x selectivity for the CB2 subtype, having a CB2 affinity of 36nM, and a CB1 affinity over 4600nM.
In animal studies it showed antipruritic effects, and passed Phase II human trials for the treatment of atopic dermatitis, but development was ultimately not continued further.[1] [2] [3] [4]
See also
Notes and References
- Odan M, Ishizuka N, Hiramatsu Y, Inagaki M, Hashizume H, Fujii Y, Mitsumori S, Morioka Y, Soga M, Deguchi M, Yasui K, Arimura A . 6 . Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent . Bioorganic & Medicinal Chemistry Letters . 22 . 8 . 2803–6 . April 2012 . 22444677 . 10.1016/j.bmcl.2012.02.072 .
- Haruna T, Soga M, Morioka Y, Hikita I, Imura K, Furue Y, Yamamoto M, Imura C, Ikeda M, Yamauchi A, Deguchi M, Shichijo M, Arimura A, Yasui K . 6 . S-777469, a novel cannabinoid type 2 receptor agonist, suppresses itch-associated scratching behavior in rodents through inhibition of itch signal transmission . Pharmacology . 2015 . 95 . 1–2 . 95–103 . 25721168 . 10.1159/000371890 . 41617054 .
- Haruna T, Soga M, Morioka Y, Imura K, Furue Y, Yamamoto M, Hayakawa J, Deguchi M, Arimura A, Yasui K . 6 . The Inhibitory Effect of S-777469, a Cannabinoid Type 2 Receptor Agonist, on Skin Inflammation in Mice . Pharmacology . 2017 . 99 . 5–6 . 259–267 . 28214870 . 10.1159/000455916 . 31692497 .
- Bow EW, Rimoldi JM . The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation . Perspectives in Medicinal Chemistry . 8 . 17–39 . 2016 . 27398024 . 4927043 . 10.4137/PMC.S32171 .