product name Almorexant
Description: Almorexant is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, 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.
512.56
Formula
C29H31F3N2O3
CAS No.
871224-64-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mM
Water: <1 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Almorexant inhibits the increase in intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat) and 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Almorexant (300 mg/kg p.o.) decreases alertness, and increases electrophysiological indices of both non-REM and REM sleep in male Wistar rats. In dogs, Almorexant (100 mg/kg p.o.) causes somnolence and increases surrogate markers of REM sleep. Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models. |
| Animal model | Wistar rats. |
| Formulation & Dosage | Dissolved in Polyethylene glycol (PEG) 400 or 0.25% methylcellulose in water; 300 mg/kg; p.o. administration |
| References | Nat Med. 2007 Feb;13(2):150-5; Neuropsychopharmacology. 2012 Sep;37(10):2210-21; Front Neurosci. 2014 Feb 25;8:33. |
