The new designer stimulant, 4-methylmethcathinone (mephedrone), most prevalently used in “Ivory Wave,” is among the most popular of the derivatives of the naturally occurring psychostimulant cathinone. Its abuse is a serious public health concern in many countries, and little about its pharmacodynamics or pharmacokinetic properties is known. Hadlock et al. evaluated the pharmacodynamics and pharmacokinetics of mephedrone to understand its mechanism of action and relationship to other abused stimulants. Similar to methylenedioxymethamphetamine (MDMA), methamphetamine (METH), and methcathinone, repeated doses of mephedrone caused a rapid decrease in striatal dopamine (DA) and hippocampal serotonin (5HT) transporter function and also inhibit synaptosomal DA and 5HT uptake; unlike METH, mephedrone caused persistent serotonergic, but not dopaminergic, deficits. Mephedrone also was self-administered by rodents, suggesting its liability for abuse. Mephedrone is a unique psychostimulant of abuse that shares pharmacological properties similar to, and yet distinct from, both METH and MDMA. Its ability to cause subjective effects reportedly resembling MDMA probably contributes to its abuse liability. These data demonstrate that mephedrone has a unique pharmacological profile with both abuse liability and neurotoxic potential.
See article at J Pharmacol Exp Ther 2011, 339:530–536
- Copyright © 2011 by The American Society for Pharmacology and Experimental Therapeutics