OX 受体拮抗剂;OX Receptor Antagonists;;InformationMK1064 MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM.Targetsorexin\u20052 receptor 18 nM
体内研究:
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.