- Almorexant
drugbox
IUPAC_name = (2"R")-2- [(1"S")-6,7-dimethoxy-1-{2- [4-(trifluoromethyl)phenyl] ethyl}-3,4-dihydroisoquinolin-2(1"H")-yl] -"N"-methyl-2-phenylacetamide
CAS_number = 871224-64-5
ATC_prefix =
ATC_suffix =
ATC_supplemental =
PubChem = 23727689
DrugBank =
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
C = 29 | H = 32 | Cl = 1 | F = 3 | N = 2 | O = 3
molecular_weight = 512.6 g/mol (free base)
bioavailability =
protein_bound =
metabolism = Hepatic
elimination_half-life =
pregnancy_category =
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routes_of_administration = OralAlmorexant (INN, codenamed ACT-078573) is a competitive antagonist of the OX1 and OX2
orexin receptors, being developed by the pharmaceutical companyActelion for the treatment of primaryinsomnia . as of|2008, it is in Phase IIIclinical trial s. [ [http://clinicaltrials.gov/ct2/show/NCT00608985 Almorexant in Adult Subjects With Chronic Primary Insomnia (RESTORA 1).] ClinicalTrials.gov (August 26, 2008). Retrieved on October 6, 2008.]Mechanism of action
Almorexant is a competitive, dual OX1 and OX2 receptor antagonist and selectively inhibits the functional consequences of OX1 and OX2 receptor activation, such as intracellular Ca2+ mobilization.
Clinical uses
Almorexant currently is under development for clinical use in primary insomnia.
ee also
*
SB-649,868 References
External links
* [http://www.actelion.com/ Actelion's official website]
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