Almorexant HCl (ACT 078573)

Description: Almorexant HCl (also known as ACT-078573; ACT078573), the hydrochloride salt of Almorexant, is a novel, potent, orally bioactive, competitive and dual orexin1/2 receptor antagonist indicated for the treatment of sleep disorders/insomnia. It inhibits OX1 and OX2 receptors with IC50s of 6.6 nM and 3.4 nM, respectively. In the inositol phosphates assay, almorexant acts as a competitive antagonist of hOX1R but a noncompetitive-like antagonist of hOX2R. Furthermore, almorexant shows effects on sleep in multiple species, including man. It reduces the time spent awake and increased the time spent in NREM and REM sleep dose-dependently in normal C57BL/6 mice. .

References: Nat Med. 2007; 13(2):150-5; Neuropsychopharmacology. 2012; 37(10):2210-21; Front Neurosci. 2014; 8:33.

Related CAS#: 871224-64-5 (free base); 913358-93-7(HCl)