5-MeO-DMT, or 5-methoxy-N,N-dimethyltryptamine, is a naturally occurring and synthetic tryptamine. It is found in some plants and animal secretions and has also been produced for research. Its pharmacology differs from DMT: it has particularly high affinity for the 5-HT1A receptor, alongside activity at 5-HT2A. Clinical studies have begun to examine its short-acting effects and potential therapeutic applications, but the evidence remains early-stage.
Chemistry and occurrence
5-MeO-DMT has a methoxy group at the 5-position of the indole ring and two methyl groups on the terminal nitrogen. It is structurally related to DMT, but the 5-methoxy substitution changes its receptor profile and metabolism. The compound occurs naturally in several biological sources, although the amount and composition vary between them.
Receptor pharmacology
5-MeO-DMT acts at multiple serotonin receptors, with particularly high affinity for 5-HT1A and activity at 5-HT2A. Reviews of cloned human receptor studies report 5-HT1A binding affinities in the low-nanomolar range. The relative contribution of 5-HT1A and 5-HT2A signalling helps explain why its effects differ from those of many classic psychedelics (Reckweg and colleagues, 2022).
Metabolism
5-MeO-DMT is metabolised mainly through oxidative deamination by monoamine oxidase A (MAO-A). A second pathway, O-demethylation by CYP2D6, produces bufotenine, which is itself pharmacologically active. Human liver and enzyme studies have shown that MAO-A activity is an important determinant of 5-MeO-DMT clearance (Shen and colleagues, 2010).
Because MAO-A is involved in its metabolism, co-administration with MAO inhibitors can substantially alter exposure. The pharmacokinetic interaction may increase and prolong serotonergic activity, which is a concern discussed in the pharmacology literature.
Human clinical research
A 2024 Phase I study examined an intranasal benzoate formulation, BPL-003, in 44 healthy volunteers. The compound was rapidly absorbed, with peak plasma concentrations reached within about 8–10 minutes and a mean terminal half-life below 27 minutes. No serious adverse events were reported; the most common events were nasal discomfort, nausea, headache and vomiting (Rucker and colleagues, 2024).
A separate randomised Phase I study published in 2025 examined repeated sublingual doses in adults with moderate symptoms of depression or anxiety. It reported transient mild side effects and no serious adverse events during the study period. These early safety findings do not establish efficacy for a psychiatric disorder or long-term safety (Bistue Millón and colleagues, 2025).
Reported effects and safety
Clinical and observational reports describe rapid changes in perception, emotional intensity and sense of self. The experience can be intense and short-lived, but its character depends on formulation and route of administration. The clinical trials used controlled settings and pharmaceutical formulations, so their findings should not be equated with unregulated products.
The relatively small human trials offer preliminary information on short-term tolerability. They do not fully establish adverse effects, interactions or long-term outcomes.
Related tryptamines
5-MeO-DMT is related to DMT, 5-Bromo-DMT, 5-MeO-MiPT and 5-MeO-DiPT. Its N,N-dimethyl side chain distinguishes it from analogues with larger alkyl groups on the terminal nitrogen.
