The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain.
European journal of pharmacology March 22, 2007 Fumiko Nagai, Ryouichi Nonaka, Kanako Satoh Hisashi Kamimura 277 citations
A new small-scale method using rat brain synaptosomes measures how psychoactive drugs affect monoamine re-uptake and release. Phenethylamine derivatives like 4-fluoroamphetamine, methylone, BDB, and MBDB strongly inhibited dopamine, serotonin, and norepinephrine re-uptake; 4-fluoroamphetamine, methylone, and BDB also strongly increased release of all three, while MBDB increased serotonin and norepinephrine release but had little effect on dopamine. Methoxylated phenethylamines (2C-I, 2C-E, 2C-C, TMA-2, TMA-6) only slightly influenced re-uptake and release. The tryptamine AMT was among the strongest re-uptake inhibitors and releasers; 5-MeO-AMT also strongly inhibited re-uptake and increased release. Other tryptamines (DPT, 5-MeO-DIPT, 5-MeO-MIPT, 5-MeO-DMT) inhibited re-uptake but had few effects on release. Piperazine derivatives 3CPP and 4MPP inhibited re-uptake and accelerated release. Results suggest some designer drugs act on the central nervous system as strongly as restricted drugs.