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Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Structurally, DMT, psilocybin (a prodrug), 5-MeO-DMT, and bufotenine are analogous to 5-HT and tryptamine. DMT is created in small amounts by the human body during normal metabolism by the enzyme tryptamine-N-methyltransferase. Like tryptamine (Airaksinen and Kari 1981; Yu et al. 2003a), tryptamine derivatives including DMT, bufotenine, and 5-MeO-DMT are excreted primarily via oxidative deamination, which is predominantly catalyzed by MAO-A (Figure 3.108) (Sanders-Bush et al. 1976; Suzuki et al. 1981; Szara and Axelrod 1959). However, there are some species differences in the metabolism of these tryptamine derivatives. DMT and 5-MeO-DMT are metabolized through deamination, N-demethylation, O-demethylation, and N-oxygenation, and N-oxide is the major metabolite in rat tissues (Sitaram et al. 1987a, b). In contrast, oxidative deamination and O-demethylation followed by glucuronidation or deamination are the major metabolic pathways for 5-MeO-DMT in rats (Agurell et al. 1969). In human liver microsomes and cultured hepatocytes, 5-MeO-DMT undergoes extensive deamination and O-demethylation, with the latter reaction being primarily catalyzed by CYP2D6 and resulting in toxic bufotenine (Yu et al. 2003c). Bufotenine is conjugated or undergoes oxidative deamination to result in 5-OH-indole acetic acid. Alternatively, bufotenine may be converted back to 5-MeO-DMT in vivo by methyltransferase. Another pathway of 5-MeO-DMT is N-oxidation, resulting in its N-oxide, which is water soluble.
5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) used in a naturalistic group setting is associated with unintended improvements in depression and anxiety
Published in The American Journal of Drug and Alcohol Abuse, 2019
Alan K. Davis, Sara So, Rafael Lancelotta, Joseph P. Barsuglia, Roland R. Griffiths
Despite these methodological limitations, these results underscore the need for further study of this psychedelic compound. When administered in a naturalistic group setting, 5-MeO-DMT appears to be associated with spontaneous and unintended improvements in self-reported depression and anxiety, which were related to more intense acute mystical effects and increases in ratings of the personal meaning and spiritual significance of the 5-MeO-DMT session, as well as higher ratings of the degree to which the session contributed to improved well-being and life satisfaction (42). Taken together, these data highlight the importance of examining the long-term effects of 5-MeO-DMT, which may enhance mood in general or may be particularly mood enhancing for those experiencing clinically significant negative affect. Davis et al (30) found that 5-MeO-DMT had a safe profile of use and low risk for health and legal consequences, but further investigation is warranted in healthy volunteers. Therefore, we recommend that studies evaluate the safety of 5-MeO-DMT using prospective experimental designs so that future studies can examine the therapeutic potential of this psychedelic substance.
Amphibious anti-depressants and other wonders
Published in The American Journal of Drug and Alcohol Abuse, 2019
5-MeO-DMT comes from many organic sources, ranging from plants, such as the ayahuasca admixture diplopterys cabrerena, to more exotic sources, such as the Sonoran Desert toad, whose parotid glands produce an exudate that may be dried, pyrolysed, and inhaled. The ceremonial use of 5-MeO-DMT likely dates back millennia, and it continues to be used in communities – both indigenous and syncretic – centered around the consumption of “plant medicines” and other “entheogens.” As reported by the authors, inhaling 5-MeO-DMT leads to profound psychoactive effects lasting about an hour, and characterized by all the hallmarks of a “psychedelic” or mystical-type state: transformations in the sense of self and of reality, and an experience of communion with a higher consciousness. The apparent lack of adverse effects is reassuring and consistent with what we know about these compounds more generally – that when administered in a responsible manner, to suitable and prepared individuals, they are almost invariably well-tolerated.
Use of Benefit Enhancement Strategies among 5-Methoxy-N,N-Dimethyltryptamine (5-MeO-DMT) Users: Associations with Mystical, Challenging, and Enduring Effects
Published in Journal of Psychoactive Drugs, 2020
Rafael L. Lancelotta, Alan K. Davis
Most reports of the benefits and negative effects of tryptamines have involved psilocybin (Araújo et al. 2015), with fewer reports published on other tryptamines (Davis et al. 2018; Winstock, Kaar, and Borschmann 2014). Of recent interest is the emerging popularity of 5-MeO-DMT as a psychedelic substance sought out for its quick onset and reportedly intense an reliably produced mystical-type experience (Psychedelics Today 2017; Sexton et al. 2019). This drug is a naturally occurring psychoactive indolealkylamine that has been shown to interact with several serotonin (5-HT) receptor subtypes, with modest selectivity as an agonist at the 5-HT1A receptor versus the 5-HT2A subtype, which is more commonly associated with psychedelic effects (Shen et al. 2010).