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Methylphenidate (Concerta/Ritalin) 54mg Tablets

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Methylphenidate (also known as MPH, MPD, and its brand names Ritalin, Concerta, and Methylin, among others) is a stimulant substance of the phenidate class. Methylphenidate is the parent compound of the substituted phenidates, a family of compounds that includes ethylphenidate, isopropylphenidate, and others. It acts primarily by enhancing the activity of the neurotransmitters dopamine and norepinephrine in the brain.

Methylphenidate was first licensed by the U.S. Food and Drug Administration (FDA) in 1955 for treating what was then known as “hyperactivity.” Although it was prescribed to patients as early as 1960, it only became heavily prescribed in the 1990s when the diagnosis of ADHD itself became more widely accepted.

Methylphenidate is approved for treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy. It is often used by students with or without ADHD to enhance their mental abilities, improve their concentration, and help them study.

SKU: RITIALIN_54MG_TABLET Category: Tags: , , ,

Chemistry

Methylphenidate is a synthetic molecule of the substituted phenethylamine and substituted phenidate classes. It contains a phenethylamine core featuring a phenyl ring bound to an amino (-NH2) group through an ethyl chain. It is structurally similar to amphetamine, featuring a substitution at Rα which is incorporated into a piperidine ring ending at the terminal amine of the phenethylamine chain. Additionally, it contains a methyl acetate bound to Rβ of its structure.

Methylphenidate is a chiral compound, presumably produced as a racemic mixture. It has an enantiopure also sold as a pharmaceutical; the dextrorotary enantiopure is known as “dexmethylphenidate” and is commonly sold as Focalin and Focalin XR.

Four isomers of methylphenidate are possible, since the molecule has two chiral centers. One pair of threo isomers and one pair of erythro are distinguished, from which primarily d-threo-methylphenidate exhibits the pharmacologically desired effects. The erythro diastereomers are pressor amines, a property not shared with the threo diastereomers. When the drug was first introduced it was sold as a 4:1 mixture of erythro:threo diastereomers, but it was later reformulated to contain only the threo diastereomers. “TMP” refers to a threo product that does not contain any erythro diastereomers, i.e. (±)-threo-methylphenidate. Since the threo isomers are energetically favored, it is easy to epimerize out any of the undesired erythro isomers. The drug that contains only dextrorotatory methylphenidate is sometimes called d-TMP, although this name is only rare usuallyly used and it is much more commonly referred to as dexmethylphenidate, d-MPH, or d-threo-methylphenidate. A review on the synthesis of enantiomerically pure (2R,2’R)-(+)-threo-methylphenidate hydrochloride has been published.

Pharmacology

Methylphenidate primarily acts as a norepinephrine-dopamine reuptake inhibitor (NDRI). It is most active at modulating levels of dopamine and, to a lesser extent, norepinephrine. Methylphenidate binds to and blocks dopamine transporters and norepinephrine transporters.

While both amphetamine and methylphenidate are dopaminergic, it should be noted that their methods of action are somewhat distinct. Specifically, methylphenidate is a dopamine reuptake inhibitor while amphetamine is both a releasing agent and reuptake inhibitor of dopamine and norepinephrine. Each of these drugs have a corresponding effect on norepinephrine which are weaker than their effects on dopamine. Methylphenidate’s mechanism of action at dopamine-norepinephrine release is still debated, but is fundamentally different from most other phenethylamine derivatives as methylphenidate is thought to increase general firing rate, whereas amphetamine reduces firing rate and reverses the flow of the monoamines via TAAR1 activation.

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