Modafinil

Inquiry

Cat Number

API0232263

CAS Number

68693-11-8

For research use only. We do not supply to patients.

For pharmaceutical-grade products or other inquiries, please contact our experts.

Product Detail Description Scientific Support Advanced Innovations Customer Q&A

CAS Number

68693-11-8

EINECS

640-968-7

Storage

Store at room temperature

Synonyms

Provigil; Modiodal; 2-(Benzhydrylsulfinyl)acetamide; 2-[(diphenylmethyl)sulfinyl]acetamide; 2-benzhydrylsulfinylacetamide; modaphonil

Molecular Formula

C15H15NO2S

Molecular Weight

273.4

Smiles

C1=CC=C(C=C1)C(C2=CC=CC=C2)S(=O)CC(=O)N

Appearance

White to off-white crystalline powder

Melting Point

164-166°C

Boiling Point

559.1±50.0°C at 760 mmHg (Predicted)

Relative Density

1.283±0.06 (Predicted)

General Description

Modafinil is a synthetic benzhydryl sulfinylacetamide derivative with a chiral center, existing as a racemic mixture of R- and S-enantiomers. Its chemical structure is 2-[(diphenylmethyl)sulfinyl]acetamide. Modafinil is a white to off-white crystalline powder, practically insoluble in water but soluble in organic solvents.

Mechanism of Action

Modafinil promotes wakefulness through multiple mechanisms, primarily by inhibiting dopamine reuptake by binding to the dopamine transporter (DAT), but with lower affinity than amphetamines. It also activates orexin (hypocretin) neurons and increases histamine, norepinephrine, and serotonin release in the hypothalamus. The drug does not cause significant euphoria or dependence, and its mechanism is unique among wake-promoting agents.

Application

Modafinil is indicated for the treatment of excessive sleepiness associated with narcolepsy, obstructive sleep apnea (as an adjunct to continuous positive airway pressure), and shift work sleep disorder. It is also used off-label for attention-deficit/hyperactivity disorder (ADHD), depression, and fatigue associated with multiple sclerosis. The drug improves wakefulness and cognitive performance without the jitteriness of traditional stimulants.

This review summarizes preclinical evidence on modafinil analogs for psychostimulant use disorder. Some analogs lack cocaine‑like effects and can blunt the reinforcing properties of psychostimulants in animal models. They show potential as pharmacotherapeutics, though further studies are needed. The review highlights the promise of modafinil derivatives in treating cocaine and methamphetamine dependence.

Fig. 1 Evaluation of the effects of JJC8–088 and JJC8–091 on self-administration or on cocaine self-administration behavior. (Tanda G, et al., 2021)

References

Tanda G, et al. Modafinil and its structural analogs as atypical dopamine uptake inhibitors and potential medications for psychostimulant use disorder. Curr Opin Pharmacol. 2021;56:13-21.

In a randomized blinded trial of 44 adults with narcolepsy type 2 or idiopathic hypersomnia, modafinil (up to 400 mg/day) and amphetamine-dextroamphetamine (up to 40 mg/day) both improved Epworth Sleepiness Scale scores (5.0 vs 4.4 points), but noninferiority of amphetamine-dextroamphetamine was not demonstrated (P=0.11). Noninferiority was shown for secondary measures of disease severity, sleepiness, and sleep inertia. Dropouts due to adverse events were higher with modafinil (31.8% vs 9.1%).

Fig. 2 Participant flow. (Trotti LM, et al., 2024)

References

Trotti LM, et al. Modafinil Versus Amphetamine-Dextroamphetamine For Idiopathic Hypersomnia and Narcolepsy Type 2: A Randomized, Blinded, Non-inferiority Trial. CNS Drugs. 2024;38(11):909-920.

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

Yes, it is photosensitive. Light exposure can cause photodegradation and discoloration of the sulfoxide group. Store in light-resistant containers, preferably amber glass.

What is the recommended storage temperature for Modafinil?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can soften the powder and accelerate racemization.

Is Modafinil hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity (>70% RH), it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity modafinil sulfone (an oxidation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains within ICH qualification thresholds.