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The R-enantiomer of pyrovalerone is devoid of activity.[4]

The primary compound of this series was 1-(methylphenyl)-2-(pyrrolidinyl)-pentanone, now more popularly known as pyrovalerone.

Amfepramone and pyrovalerone are in Schedule IV of that Convention, but other derivatives are not under international control.

Pyrovalerone (and by extension, its derivatives) is a structural relative of the CNS stimulant cathinone, and can therefore be referred to as a substituted cathinone.

In 1969, the methylenedioxyphenyl analogue of pyrovalerone, now well known by the abbreviation MDPV, was patented by a pharmaceutical company known by Boehringer Ingelheim.