Suvorexant

Inquiry

Cat Number

API0231546

CAS Number

1030377-33-3

If you have any other questions, please contact our experts.

Product Detail Description Scientific Support Customer Q&A

CAS Number

1030377-33-3

EINECS

685-109-7

Storage

Store at room temperature

Synonyms

MK-4305; BELSOMRA; [(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

Molecular Formula

C23H23ClN6O2

Molecular Weight

450.9

Smiles

C[C@@H]1CCN(CCN1C(=O)C2=C(C=CC(=C2)C)N3N=CC=N3)C4=NC5=C(O4)C=CC(=C5)Cl

Appearance

Off-white powder

General Description

Suvorexant is a first-in-class dual orexin receptor antagonist approved for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. It is available in oral tablet form and represents a novel mechanism distinct from traditional sedative-hypnotics such as benzodiazepines and Z-drugs. The drug selectively targets the orexin neuropeptide signaling system that promotes wakefulness.

Mechanism of Action

Suvorexant competitively antagonizes both orexin receptor type 1 (OX1R) and orexin receptor type 2 (OX2R), which are activated by the wake-promoting neuropeptides orexin A and B. By blocking orexin signaling in the hypothalamus and other wake-promoting brain regions, suvorexant reduces arousal drive and facilitates the transition to and maintenance of sleep. This mechanism preserves more physiological sleep architecture compared to non-selective GABAergic sedatives.

Application

It is indicated for the treatment of insomnia in adults, specifically for patients who have difficulty falling asleep or staying asleep. Unlike traditional hypnotics, suvorexant is not associated with tolerance or withdrawal at therapeutic doses, though next-morning somnolence and impaired driving ability are important safety considerations. It is classified as a controlled substance (Schedule IV) due to potential for abuse, and the recommended dose is 10 to 20 mg taken within 30 minutes of bedtime.

This study examined the dual orexin receptor antagonist suvorexant in rodent models of cocaine use disorder. Suvorexant (i) decreased the number of cocaine infusions earned under a progressive‑ratio schedule, indicating reduced motivation; (ii) attenuated initial positive hedonic reactivity to cocaine (measured by 50‑kHz ultrasonic vocalizations) and prevented cocaine place preference; (iii) did not affect cocaine‑induced hyperlocomotion; and (iv) reduced cocaine‑evoked increases in extracellular ventral striatal dopamine. The findings support the therapeutic potential of orexin receptor antagonists for treating cocaine use disorder, likely through modulation of mesolimbic dopamine signaling.

Fig. 1 Effects of suvorexant on cocaine-induced locomotor activity. (Gentile TA, et al., 2018)

References

Gentile TA, et al. Suvorexant, an orexin/hypocretin receptor antagonist, attenuates motivational and hedonic properties of cocaine. Addict Biol. 2018; 23(1):247-255.

Does Suvorexant require protection from light during long-term storage?

Yes, it is photosensitive. Prolonged exposure to UV light can cause photodegradation and impurity formation. Store in light-resistant containers, preferably in original amber glass or opaque packaging.

What is the recommended storage temperature for Suvorexant?

Store at controlled room temperature (15-25°C). It is thermally stable, but avoid temperatures above 30°C to prevent potential polymorphic changes or softening.

Is Suvorexant hygroscopic, and how is this managed?

It exhibits low to moderate hygroscopicity. We recommend storage in tightly sealed containers with desiccant, especially in climates with relative humidity above 60%.

How is the enantiomeric purity of Suvorexant maintained during storage?

We use chiral HPLC to monitor the (R)-enantiomer, confirming that no racemization occurs under recommended storage conditions throughout the product's shelf life.