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GLOSSARY · DMT AND AYAHUASCA

5-MeO-DMT

Also called: 5-methoxy-DMT

DMT with one extra methoxy group on the ring, which makes it a different drug. It binds most strongly to the 5-HT1A receptor, and in Canada it is not named in the drug schedules; its sale falls under the Food and Drugs Act.

Full article: What is 5-MeO-DMT? The molecule, the research and the law in Canada

5-MeO-DMT (5-methoxy-N,N-dimethyltryptamine, also called mebufotenin) is a short-acting psychedelic tryptamine. It is found in the Sonoran Desert toad’s secretion and in small amounts in some plants. One extra methoxy group separates it from DMT, and that change makes it a different drug.

Most classic psychedelics work mainly through the 5-HT2A receptor. A 2022 review reports that 5-MeO-DMT binds most strongly to the 5-HT1A receptor, with 300 to 1,000-fold higher selectivity for it than for 5-HT2A (Reckweg et al., 2022). Studies describe a loss of the sense of self with comparatively little visual imagery, and researchers suspect the 5-HT1A tilt is part of the reason; that has not been shown directly.

A synthetic inhaled form, GH001, is in clinical trials. In a phase 2b trial of 81 adults with treatment-resistant depression, 57.5% on GH001 were in remission at day 8, against none on placebo, and effects lasted a median of 9 to 14 minutes (Cubała et al., 2026). It is not an approved medicine.

In Canada, 5-MeO-DMT is not named in the Controlled Drugs and Substances Act. Health Canada uses it as its example of a new psychoactive substance whose sale is regulated under the Food and Drugs Act (Health Infobase). Not scheduled is not the same as approved or safe. This is not legal advice.

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