Pharmacology of “replacement” analogs of mephedrone and methylone
Michael H. Baumann, Kurt R. Lehner, M. Omar Bukhari and John S. Partilla
Designer Drug Research Unit (DDRU),
Intramural Research Program, NIDA, NIH
Baltimore, MD 21224
In recent times, there has been an alarming increase in the abuse of synthetic stimulants such as 4-methyl-N-methylcathinone (mephedrone) and 3,4-methylenedioxy-N-methylcathinone (methylone). Due to public health risks, these drugs have been rendered illegal by legislative bans in the US and Europe, but new “replacement” cathinones are appearing in the recreational drug marketplace. Here, we will describe in vitro and in vivo effects of replacement analogs of mephedrone and methylone. All of the newer cathinones target monoamine transporter proteins as either blockers (i.e., cocaine-like drugs) or substrates (i.e., amphetamine-like drugs). However, subtle changes in drug structure can have profound effects on the precise mechanism of action, and the relative selectivity for dopamine versus serotonin transporters, yielding a rich pharmacology.