Almorexant-13C-d3 is intended for use as an internal standard for the quantification of almorexant by GC- or LC-MS. Almorexant is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 4.7 and 0.9 nM, respectively, in a radioligand binding assay).1 It decreases the latency to persistent non-rapid eye movement (NREM) sleep and increases the duration of NREM and REM sleep in male rats when administered at a dose of 100 mg/kg.2 Almorexant (300 mg/kg) does not impair spatial learning and memory in the Morris water maze and does not reverse spatial memory impairments induced by scopolamine in rats.3
|1. Malherbe, P., Borroni, E., Pinard, E., et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: Comparison with selective OX1 and OX2 antagonists. Molecular Pharmacology 76(3), 618-631 (2015).|2. Brisbare-Roch, C., Dingemanse, J., Koberstein, R., et al. Promotion of sleep by targeting the orexin system in rats, dogs and humans. Nat. Med. 13(2), 150-155 (2007).|3. Dietrich, H., and Jenck, F. Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl.) 212(2), 145-154 (2010).