IPSU是一款具有选择性、口服活性和脑渗透性的OX2R拮抗剂,其pKi值为7.85。
[1] Callander GE, Olorunda M, Monna D, Schuepbach E, Langenegger D, Betschart C, Hintermann S, Behnke D, Cotesta S, Fendt M, Laue G, Ofner S, Briard E, Gee CE, Jacobson LH, Hoyer D. Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. doi: 10.3389/fnins.2013.00230. PMID: 24376396; PMCID: PMC3847553.[2]Betschart C, Hintermann S, Behnke D, Cotesta S, Fendt M, Gee CE, Jacobson LH, Laue G, Ofner S, Chaudhari V, Badiger S, Pandit C, Wagner J, Hoyer D. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607. doi: 10.1021/jm4007627. Epub 2013 Sep 18. PMID: 23964859.





