Almorexant

Almorexant
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Systematic (IUPAC) name
(2R)-2-[(1S)- 6,7-dimethoxy- 1-{2-[4-(trifluoromethyl)phenyl]ethyl}- 3,4-dihydroisoquinolin-2(1H)-yl]- N-methyl- 2-phenylacetamide
Identifiers
CAS number 871224-64-5
ATC code None
PubChem CID 23727689
Chemical data
Formula C29H32ClF3N2O3 
Mol. mass 512.6 g/mol (free base)
SMILES eMolecules & PubChem
Pharmacokinetic data
Metabolism Hepatic
Therapeutic considerations
Pregnancy cat.  ?
Legal status  ?
Routes Oral

Almorexant (INN, codenamed ACT-078573) is a competitive receptor antagonist of the OX1 and OX2 orexin receptors, being developed by the pharmaceutical company Actelion for the treatment of primary insomnia. It has completed a Phase III clinical trial in November 2009.[1]

Contents

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.

See also

References

  1. Almorexant in Adult Subjects With Chronic Primary Insomnia (RESTORA 1). ClinicalTrials.gov (February 3, 2010). Retrieved on May 6, 2010.

External links

Template:Hypnotics and sedatives Template:Neuropeptide agonists and antagonists

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