Inhibitory effect of 5-methoxy-N,N-dimethyltryptamine on the synaptosomal uptake of 5-hydroxytryptamine.
European journal of pharmacology June 3, 1983 DOI: 10.1016/0014-2999(83)90253-4 via PubMed
Summary
AI-generated from the abstract5-MeO-DMT, a psychedelic compound, inhibits the reuptake of serotonin in rat brain tissue at concentrations between 0.5 and 500 micromolar, affecting the striatum, hippocampus, and hypothalamus. At higher concentrations (10 micromolar), it also inhibits dopamine reuptake and triggers the release of both serotonin and dopamine from nerve endings. These findings suggest that 5-MeO-DMT's effects as a serotonin agonist may involve blocking reuptake, not just directly stimulating receptors as previously thought.
Study at a glance
| Characteristics | In vitro study Peer reviewed |
|---|---|
| Population | Rat brain synaptosomes |
| Intervention | 5-MeODMT |
| Dose | 0.5-500 microM for uptake inhibition; 10 microM for release and dopamine uptake inhibition |
| Citations | 20 |
| Key finding | 5-MeO-DMT inhibits serotonin and dopamine reuptake and induces their release in rat brain synaptosomes, indicating its agonist properties may involve reuptake inhibition. |
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.