Methylphenidate

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Cat Number

API0233293

CAS Number

113-45-1

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Product Detail Description Scientific Support Customer Q&A

CAS Number

113-45-1

EINECS

204-028-6

Synonyms

Methylphenidan, Phenidylate, Calocain

Molecular Formula

C14H19NO2

Molecular Weight

233.31

Smiles

COC(=O)C(C1CCCCN1)C2=CC=CC=C2

General Description

Methylphenidate is a central nervous system stimulant derived from phenethylamine and used primarily for attention deficit hyperactivity disorder and narcolepsy.

Mechanism of Action

Methylphenidate acts as a norepinephrine and dopamine reuptake inhibitor, blocking the transporters for these neurotransmitters and increasing their concentration in the synaptic cleft. It is a racemic mixture of d- and l-isomers, with the d-isomer being more pharmacologically active.

Application

Methylphenidate is FDA-approved for the treatment of attention deficit hyperactivity disorder in children aged 6 years and older and adults, and as a second-line treatment for narcolepsy.

Faraone SV. compared the distinct pharmacologic mechanisms of amphetamine and methylphenidate, the first-line psychostimulants used for attention-deficit/hyperactivity disorder (ADHD). Both drugs increase central dopamine and norepinephrine activity, thereby impacting executive function and attention, but they do so through different molecular actions. Amphetamine inhibits dopamine and norepinephrine transporters, inhibits vesicular monoamine transporter 2 (VMAT-2), and inhibits monoamine oxidase. Methylphenidate inhibits dopamine and norepinephrine transporters, exhibits agonist activity at serotonin 5-HT₁A receptors, and redistributes VMAT-2.

Fig. 1 PRISMA flow diagram of the literature search (Faraone SV, 2018)

References

Faraone SV. The pharmacology of amphetamine and methylphenidate: Relevance to the neurobiology of attention-deficit/hyperactivity disorder and other psychiatric comorbidities. Neurosci Biobehav Rev. 2018;87:255-270.

What are the specific storage requirements for Methylphenidate as a controlled substance?

As a Schedule II CNS stimulant, it must be stored in a securely locked, limited-access area with complete inventory records, in compliance with DEA and international regulations.

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

Yes, it is photosensitive. Storage in light-resistant, amber or opaque containers is recommended to prevent photodegradation and maintain its purity.

What is the recommended storage temperature for Methylphenidate?

Store at controlled room temperature, between 15°C and 25°C. Avoid excessive heat, which can soften the material and accelerate degradation.

Is Methylphenidate prone to racemization during storage?

The threo isomer is stable under recommended conditions. We monitor chiral purity using a validated chiral HPLC method to ensure no racemization occurs over time.