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ACS Chem Neurosci. 2016 Aug 17;7(8):1030-40. doi: 10.1021/acschemneuro.6b00199. Epub 2016 Jul 25.

Classics in Chemical Neuroscience: Methylphenidate.

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  • 1Department of Chemistry, The Scripps Research Institute , La Jolla, California 92037, United States.


As the first drug to see widespread use for the treatment of attention deficit hyperactivity disorder (ADHD), methylphenidate was the forerunner and catalyst to the modern era of rapidly increasing diagnosis, treatment, and medication development for this condition. During its often controversial history, it has variously elucidated the importance of dopamine signaling in memory and attention, provoked concerns about pharmaceutical cognitive enhancement, driven innovation in controlled-release technologies and enantiospecific therapeutics, and stimulated debate about the impact of pharmaceutical sales techniques on the practice of medicine. In this Review, we will illustrate the history and importance of methylphenidate to ADHD treatment and neuroscience in general, as well as provide key information about its synthesis, structure-activity relationship, pharmacological activity, metabolism, manufacturing, FDA-approved indications, and adverse effects.


ADHD; Methylphenidate; Ritalin; history; hyperkinetic disorder; stimulant

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