Suvorexant Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Suvorexant, a dual orexin receptor antagonist marketed under the trade name Belsomra®, discovered and developed by Merck for the treatment of insomnia, was approved by the US FDA in August 2014 and became available in Japan in November of the same year. The drug’s mechanism of action operates through the competitive blockade of wake-promoting neuropeptides orexin A and orexin B toward receptors orexin receptor type 1 and orexin receptor type 2, which are believed to modulate sleep-wake cycles.

Verwenden

Suvorexant (MK-4305) is a dual (non-selective) orexin receptor antagonist in development by Merck & Co. for the treatment of insomnia. It works by turning off wakefulness rather than by inducing sleep. Users of higher doses had an increased rate of suicidal ideation.

Definition

ChEBI: Suvorexant is an aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia. It has a role as a central nervous system depressant and an orexin receptor antagonist. It is a member of 1,3-benzoxazoles, a member of triazoles, a diazepine, an aromatic amide and an organochlorine compound.

Biologische Aktivit?t

Suvorexant is a dual orexin receptor (OXR) antagonist that blocks both OX1R and OX2R (Kis = 1.2 and 0.60 nM, respectively). It reduces locomotor activity and promotes sleep by inhibiting the binding of orexin A and B. In rats, suvorexant decreases self-administration of, and conditioned place preference for, cocaine ( | 16186 | ISO60176). It also decreases dopamine levels in the rat ventral striatum following a cocaine-induced increase. Formulations containing suvorexant are used in the treatment of insomnia.  Suvorexant is regulated as a Schedule IV compound in the United States. This compound is also available as an analytical reference standard.

Stoffwechsel

Suvorexant is primarily metabolized by cytochrome-P450 3A4 enzyme (CYP3A4) with a minor contribution from CYP2C19. Major circulating metabolites are suvorexant and a hydroxy-suvorexant metabolite, which is not expected to be pharmacologically active. There is potential for drug-drug interactions with drugs that inhibit or induce CYP3A4 activity.

Suvorexant Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

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• 5-Chloro-2-[(5R)-5-methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole
• MK 4305
• Suvorexant
• MK-4305 (Suvorexant)
• Methanone, [(7R)-4-(5-chloro-2-benzoxazolyl)hexahydro-7-Methyl-1H-1,4-diazepin-1-yl][5-Methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]-
• Suvorexant (MK-4305)
• Suvorexant (with 4 ints.)
• SUVOREXABT
• Synonyms Suvorexant
• MK-4305, >=98%
• 5-Chloro-2-[(5R)-5-methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole MK 4305
• SUVOREXANT (MK-4305);MK-4305
• MK-4305 cas 1030377-33-3 Suvorexant powder kf-wang(at)kf-chem.com
• EOS-61934
• [(7R)-4-(5-CHLORO-1,3-BENZOXAZOL-2-YL)-7-METHYL-1,4-DIAZEPAN-1-YL][5-METHYL-2-(2H-1,2,3-TRIAZOL-2-YL)PHENYL]METHANONE
• CID24965990
• Suvorexant USP/EP/BP
• (R)-(4-(5-chlorobenzo[d]oxazol-2-yl)-7-Methyl-1,4-diazepan-1-yl)(5-Methyl-2-(2H-1,2,3-triazol-2-yl)phenyl)Methanone
• 5-Chloro-2-[(5R)-5-methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl]-1,3-benzoxazole Suvorexant (MK-4305)
• Suvorexan
• 3-Pyridinecarboxaldehyde,2,10-dichloro-
• (7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1H-1,4-diazepin-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone
• 13C6]-Suvorexant
• 5-Chloro-2- [(5R) -5-methyl-4- [5-methyl-2- (2H-1,2,3-triazol-2-yl) benzoyl] -1,4-diazocycloheptane-1-yl] -1,3-benzoxazole
• MK4305 MK-4305
• Suvorexant(control)
• 1030377-33-3
• 030377-33-3
• C23H23ClN6O2
• API
• Inhibitors
• 1030377-33-3