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

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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 =
legal_status =
routes_of_administration = Oral

Almorexant (INN, codenamed ACT-078573) is a competitive antagonist of the OX₁ and OX₂ orexin receptors, being developed by the pharmaceutical company Actelion for the treatment of primary insomnia. as of|2008, it is in Phase III clinical trials. [ [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]