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It is a stimulant drug related to cathinone and methcathinone. The effects of Mephedrone are reportedly comparable to those of similar drugs such as MDMA and methylone.

Mephedrone is an inhibitor of monoamine transporter present in the brain and periphery. Mephedrone bears a chiral center and can be found in two enantiomers R-mephedrone and S-mephedrone. Its racemic form is often used as a drug. Mephedrone in rats is known to cause high blood pressure and heart rate, as well as stimulates locomotor hyperactivity. Human trail reveal that mephedrone has the ability to induce euphoria and pleasure.