Suvorexant

한글명:Suvorexant

카스 번호1030377-33-3

상품명:Suvorexant

CBNumberCB62589660

분자식C23H23ClN6O2

포뮬러 무게450.92

MOL 파일1030377-33-3.mol

화학적 성질

녹는점	153℃
끓는 점	669.8±65.0 °C(Predicted)
밀도	1.41
저장 조건	Room Temperature
용해도	아세토니트릴(약간 용해됨), 클로로포름(약간 용해됨), DMSO(약간 용해됨, 가열)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	1.47±0.40(Predicted)
색상	흰색에서 옅은 베이지까지
InChIKey	JYTNQNCOQXFQPK-MRXNPFEDSA-N
SMILES	C(N1[C@H](C)CCN(C2=NC3=CC(Cl)=CC=C3O2)CC1)(C1=CC(C)=CC=C1N1N=CC=N1)=O

위험 및 안전 성명

DEA Controlled Substances

CSCN: 2223
CAS SCH: IV
NARC: N

그림문자(GHS)

Suvorexant 화학적 특성, 용도, 생산

개요
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.
용도
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.
정의
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.
생물학적 활성
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.
신진 대사
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.

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