DMT is an how to release dmt that has both botanical roots and a rich archaic cultural history of medicinal use, along with psilocybin, as psychoactive ethnobotanical medicines in South America. It is found in the tisanes (infusions) known as yage, ayahuasca and hoasca, that are consumed for spiritual purposes and therapeutic treatment in indigenous South American cultures.

Unlike many other psychedelics, DMT is not metabolized by monoamine oxidase (MAO). It is therefore able to pass directly from the bloodstream into brain cells and exert its effects without interference from MAO or its metabolites. This is one reason why DMT has been such a central topic in psychedelic research and therapeutics.

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However, the rapid metabolism and clearance of peripherally administered DMT by MAO can lead to an incomplete picture of its potential pharmacology. For example, a number of DMT metabolites have been shown to exhibit hallucinogenic effects that differ from those observed with DMT alone (Nichols and Szabo, 2017).

The need to develop an oral route of administration for DMT that resists metabolism without necessitating the concomitant use of an MAOI while retaining its potency and efficacy for the desired treatment has generated considerable interest in the harmala alkaloids. Several different strategies for resisting MAO-mediated metabolism of DMT have been investigated, including changing the side chain nitrogen of DMT by substituting it with an alkyl group that does not interact with MAO. Selection of the proper substitution(s) for this nitrogen may also have a major impact on binding properties at the 5HT2a receptor, which is the primary target of DMT metabolism by MAO.