1233932-22-3Relevant articles and documents
Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists
Fujimoto, Tatsuhiko,Tomata, Yoshihide,Kunitomo, Jun,Hirozane, Mariko,Marui, Shogo
, p. 6409 - 6413 (2011/11/29)
To generate novel human Orexin-2 Receptor (OX2R) antagonists, a spiropiperidine based scaffold was designed and a SAR study was carried out. Compound 4f possessed the highest OX2R antagonistic activity with an IC 50 value of 3 nM with 450-fold selectivity against Orexin-1 Receptor (OX1R).