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.

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 (2019) 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. J Med Chem 62(3):1203-1217. doi: 10.1021/acs.jmedchem.8b01280

Objective: To discover and develop a therapeutic for human sleep disorders.

Summary: Histamine H3 Receptor Inverse Agonist demonstrated high receptor occupancy and marked wake promoting effects with decreased REM sleep in Orexin-B-SAP lesioned rats. This study supports its potential therapeutic utility in treating human sleep disorders.

Usage: Injections (490 ng/0.8 μl) were made bilaterally to the lateral hypothalamus.

Related Products: Orexin-B-SAP (Cat. #IT-20)