[8][9][10][11] It is an unusual and unique DRI, acting as a negative allosteric modulator and non-competitive inhibitor of the dopamine transporter (DAT).

[8][9][10] Chemically, mesocarb contains amphetamine within its structure but has been modified and extended at the amine with a sydnone imine-containing moiety.

[16] Mesocarb was originally developed in the Soviet Union in the 1970s[17][18] for a variety of indications including asthenia, apathy, adynamia, and some clinical aspects of depression and schizophrenia.

[19][20] Mesocarb was used for counteracting the sedative effects of benzodiazepines,[21] increasing workload capacity and cardiovascular function,[22] treatment of attention deficit hyperactivity disorder (ADHD) in children,[23][24] as a nootropic,[25] and as a drug to enhance resistance to extremely cold temperatures.

[10] In 2021, it was discovered that mesocarb is not a conventional DRI but acts as a DAT allosteric modulator or non-competitive inhibitor.

Subsequently, with the advent of mass spectroscopy, it has been shown that presence of amphetamine in prior studies was an artifact of the gas chromatography method.

[35] More recent studies using mass spectroscopy show that negligible levels of amphetamine are released from mesocarb metabolism.

[7] Mesocarb is almost unknown in the western world and is neither used in medicine nor studied scientifically to any great extent outside of Russia and other countries in the former Soviet Union.

It has however been added to the list of drugs under international control and is a scheduled substance in most countries, despite its multiple therapeutic applications and reported lack of significant abuse potential.