MK-1064

A potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki/IC50 of 0.5/18 nM; displays >100-fold selectivity over OX1R; promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats and dogs without inducing cataplexy; also decreases ACTH levels in rats.Sleep Disorder Preclinical (In Vitro) :MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice.MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats.MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey.