Inhibitory effect of 5-methoxy-N,N-dimethyltryptamine on the synaptosomal uptake of 5-hydroxytryptamine.
European journal of pharmacology – June 03, 1983
Source: PubMed
Summary
5-Methoxy-N,N-dimethyltryptamine (5-MeODMT) significantly inhibits serotonin uptake in rat brain synaptosomes, with a notable effect at 10 microM concentrations. Specifically, it reduced [14C]serotonin uptake by over 50% across striatal, hippocampal, and hypothalamic regions. Additionally, 5-MeODMT prompted the release of both serotonin and dopamine from preloaded synaptosomes, suggesting that its effects may stem from reuptake inhibition alongside direct receptor stimulation. These findings highlight the complex role of 5-MeODMT in neurotransmitter dynamics within the brain.
Abstract
5-Methoxy-N,N-dimethyltryptamine (5-MeODMT) in concentrations of 0.5-500 microM produced a significant inhibition of [14C]5-hydroxytryptamine [14C]5-HT) uptake in striatal, hippocampal and hypothalamic crude synaptosomes from rat brain. Higher concentrations of 5-MeODMT (10 microM) also inhibited the uptake of [3H]dopamine [3H]DA) and induced the release of [14C]5-HT and [3H]DA from preloaded synaptosomes. It appears that the 5-HT agonist properties of 5-MeODMT may involve reuptake inhibition in addition to the previously documented direct receptor stimulation.