Neurotoxicity of the psychedelic amphetamine, methylenedioxymethamphetamine.
Journal of Pharmacology and Experimental Therapeutics January 1, 1987 C J Schmidt 530 citations
The psychedelic agent MDMA may be a serotonergic neurotoxin similar to p-chloroamphetamine. MDMA produced a biphasic effect on cortical serotonin concentrations: an acute depletion peaking 3 to 6 hours after administration that reversed within 24 hours, followed by a second depletion phase one week later. This later phase involved a decrease in synaptosomal serotonin uptake due to fewer uptake sites, with no change in carrier affinity. The neurotoxic effect was specific to the (+)-stereoisomer, while both isomers caused acute depletion. Coadministration of the serotonin uptake inhibitor fluoxetine completely blocked the long-term reduction in serotonin, and partial blockade occurred even when fluoxetine was given up to 6 hours after MDMA.