Almorexant HCl (C09-0735-180)

InformationAlmorexant HCl (ACT-078573) is an orally active, dualorexin receptorantagonist withIC50of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.TargetsOX2 receptor ; OX1 receptor 3.4 nM; 6.6 nMIn vitroAlmorexant 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.In vivoAlmorexant (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. Specification: 0.98 Molecular Formula: C29H32ClF3N2O3 Molecular Weight: 549.02 PubChem CID: 25227440 Isomeric SMILES: CNC(=O)[C@@H](C1=CC=CC=C1)N2CCC3=CC(=C(C=C3[C@@H]2CCC4=CC=C(C=C4)C(F)(F)F)OC)OC.Cl Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/A412771-SCI_f3dccdcbf20848394610738456fadadd.pdf