Orexin-SAP Model of Sleep Disorders

Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-Yloxy)Phenyl]-2-(Morpholin-4-Yl)Acetamide Dihydrochloride (Suvn-G3031): A Novel, Potent, Selective, and Orally Active Histamine H3 Receptor Inverse Agonist with Robust Wake-Promoting Activity. (2019). J Med Chem, 62 (3):1203-1217. Nirogi R, Shinde A, Mohammed AR, Badange RK, Reballi V, Bandyala TR, Saraf SK, Bojja K, Manchineella S, Achanta PK, Kandukuri KK, Subramanian R, Benade V, Palacharla RC, Jayarajan P, Pandey S, & Jasti V.

IT-20:  Orexin-SAP

Objective:  To examine the effects of clinical candidate, 17v on sleep/wake activity in Orexin-SAP lesioned male Wistar rats.
Summary:  17v demonstrated high receptor occupancy and marked wake-promoting effects with decreased rapid-eye-movement sleep in Orexin-SAP lesioned rats supporting its potential therapeutic utility in treating human sleep disorders.
Dose:  Intracerebral injections of Orexin-SAP (100 ng/0.5 μl) in lateral hypothalamus of rats produce selective disruption of neurons containing orexin-B receptors and produces symptoms that are characteristic of narcolepsy.

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