Effects of Certain Hallucinogenic Amphetamine Analogues on the Release of Serotonin from Rat Brain Synaptosomes

Article abstract of DOI:10.1021/jm00347a010

The enantiomers of 3,4-(methylenedioxy)amphetamine (MDA), p-methoxyamphetamine (PMA), and N-Me-MDA (MDMA), along with their α,α-dimethylated derivatives, were evaluated for an effect on the release of <3H>serotonin from rat whole brain synaptosomes.The amphetamine isomers were all potent in inducing the release of <3H>serotonin at bath concentrations of 1 and 10 μM but were inactive at 0.1 μM.No significant difference in isomer potency was observed at the 10-μM concentration.However, at 1 μM the (+) isomer of MDMA was more effective in inducing release than was the (-) isomer.Since it is the (+) isomer which is clinically active, this result suggests that transmitter release may play a role in the biological activity of MDMA.By contrast, the α,α-dimethyl compounds were not effective in releasing serotonin, even at the highest bath concentration.