Orexin 2 Receptor Agonist

Description: Orexin 2 Receptor Agonist is a potent and selective Orexin2 receptor agonist with EC50 of 0.023 uM on OX2R; it is OX2R-selective (OX1R/OX2R EC50 ratio is 70). Orexins are a family of neuropeptides that regulate sleep/wakefulness, acting on two G-protein-coupled receptors, orexin receptors 1 (OX1R) and 2 (OX2R). Genetic and pharmacologic evidence suggests that orexin receptor agonists, especially OX2R agonist, will be useful for mechanistic therapy of the sleep disorder narcolepsy/cataplexy. We herein report the discovery of a potent (EC50 on OX2R is 0.023 uM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist, 4'-methoxy-N, N-dimethyl-3'-N-(3-{2-(3-methylbenzamido)ethylamino}phenyl)sulfamoyl-(1, 1'-biphenyl)-3-carboxamide 26.

References: J Med Chem. 2015 Oct 22; 58(20):7931-7.