Almorexant (hydrochloride)

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). 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. 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.Formal Name: (alphaR,1S)-3,4-dihydro-6,7-dimethoxy-N-methyl-alpha-phenyl-1-[2-[4-(trifluoromethyl)phenyl]ethyl]-2(1H)-isoquinolineacetamide, monohydrochloride. CAS Number: 913358-93-7. Synonyms: ACT 078573. Molecular Formula: C29H31F3N2O3 . HCl. Formula Weight: 549.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 285 nm. SMILES: O=C(NC)[C@@H](C1=CC=CC=C1)N2CCC3=C(C=C(OC)C(OC)=C3)[C@@H]2CCC4=CC=C(C(F)(F)F)C=C4. InChi Code: InChI=1S/C29H31F3N2O3/c1-33-28(35)27(20-7-5-4-6-8-20)34-16-15-21-17-25(36-2)26(37-3)18-23(21)24(34)14-11-19-9-12-22(13-10-19)29(30,31)32/h4-10,12-13,17-18,24,27H,11,14-16H2,1-3H3,(H,33,35)/t24-,27+/m0/s1. InChi Key: DKMACHNQISHMDN-RPLLCQBOSA-N.