Orexin antagonist

An orexin receptor antagonist is a drug that inhibits the effect of orexin by acting as a receptor antagonist of the orexin receptor. Potential applications include treatment of sleep disorders such as insomnia.[1][2]

Examples

Almorexant, development of the drug was abandoned in January 2011
Lemborexant
Nemorexant
Filorexant
SB-334,867, has been shown to produce sedative and anorectic effects in animals,[3]
SB-408,124
SB-649,868, in development for potential use in sleep disorders
Suvorexant, approved for use in sleep disorders under the brand name Belsomra
TCS-OX2-29, OX₂ selective
RTIOX-276, OX₁ selective

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References

Roecker AJ, Coleman PJ (2008). "Orexin receptor antagonists: medicinal chemistry and therapeutic potential". Curr Top Med Chem. 8 (11): 977–87. doi:10.2174/156802608784936746. PMID 18673167.
Cao M, Guilleminault C (April 2011). "Hypocretin and its emerging role as a target for treatment of sleep disorders". Curr Neurol Neurosci Rep. 11 (2): 227–34. doi:10.1007/s11910-010-0172-9. PMID 21170610.
Rodgers RJ, Halford JC, Nunes de Souza RL, Canto de Souza AL, Piper DC, Arch JR, Upton N, Porter RA, Johns A, Blundell JE (April 2001). "SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats". Eur. J. Neurosci. 13 (7): 1444–52. doi:10.1046/j.0953-816x.2001.01518.x. PMID 11298806.

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[pmid18673167-1] Roecker AJ, Coleman PJ (2008). "Orexin receptor antagonists: medicinal chemistry and therapeutic potential". Curr Top Med Chem. 8 (11): 977–87. doi:10.2174/156802608784936746. PMID 18673167.

[pmid21170610-2] Cao M, Guilleminault C (April 2011). "Hypocretin and its emerging role as a target for treatment of sleep disorders". Curr Neurol Neurosci Rep. 11 (2): 227–34. doi:10.1007/s11910-010-0172-9. PMID 21170610.

[pmid11298806-3] Rodgers RJ, Halford JC, Nunes de Souza RL, Canto de Souza AL, Piper DC, Arch JR, Upton N, Porter RA, Johns A, Blundell JE (April 2001). "SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats". Eur. J. Neurosci. 13 (7): 1444–52. doi:10.1046/j.0953-816x.2001.01518.x. PMID 11298806.