Almorexant

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Almorexant
File:Almorexant.svg
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
Clinical data
Routes of
administration		 Oral
Pharmacokinetic data
Metabolism Hepatic
Identifiers
CAS Number 871224-64-5
ATC code none
PubChem CID 23727689
Chemical data
Formula C29H32ClF3N2O3
Molar mass 512.6 g/mol (free base)[[Script error: No such module "String".]]
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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]

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

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External links

GABAA receptor
Ultrashort-acting
Short/intermediate-
acting
Long-acting
Ungrouped
Short-acting
Intermediate-acting
Long-acting
Dialkylphenols
Alpha-2 adrenergic
receptor
Melatonin receptor
Histamine receptor &
Acetylcholine receptor
5-HT2A &
α1-adrenergic
Selective 5-HT2A & α1-adrenergic antagonists
GABAB receptor /
GHB receptor
GHB Type
Orexin receptors
Orexin antagonists
Almorexant • SB-334,867 • SB-408,124 • SB-649,868 • TCS-OX2-29
Other receptors/
ungrouped
Other

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc, drug(N5A/5B/5C/6A/6B/6D)


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