ACS Medicinal Chemistry Letters
July 10, 2026
Anna C. Renner, Robert B. Kargbo
The psychedelic therapeutics field is moving beyond classical hallucinogens to integrated treatment platforms that combine optimized pharmacology, drug delivery, and clinical implementation. Recent patent applications describe selective 5-HT2A receptor activators, precision aerosol delivery technologies for psychedelic compounds, and structured 5-MeO-DMT treatment regimens for depression. These innovations represent a convergence toward scalable, safer, and clinically practical neuropsychiatric therapies that may reshape the future of serotonergic medicine.
Psychopharmacology (Berl)
April 13, 2019
M. V. Uthaug, R. Lancelotta, K. Van Oorsouw et al.
198 citations
A single inhalation of vapor from dried toad secretion containing 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) in a naturalistic setting is associated with sustained improvements in life satisfaction and mindfulness-related capacities, along with a reduction in psychopathological symptoms.
PloS one
January 1, 2014
Attila Szabo, Attila Kovács, Ede Frecska et al.
191 citations
The sigma-1 receptor, a protein found in the central nervous system and immune cells, can be activated by the psychedelic compounds N,N-dimethyltryptamine (NN-DMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) to dampen inflammatory responses in human immune cells. When human dendritic cells were exposed to inflammatory triggers along with these compounds, production of pro-inflammatory cytokines IL-1β, IL-6, TNFα, and chemokine IL-8 decreased, while the anti-inflammatory cytokine IL-10 increased. The compounds also reduced the cells' ability to activate inflammatory T-cells. This suggests dimethyltryptamines may act as endogenous regulators of inflammation and immune balance, pointing toward potential treatments for autoimmune and chronic inflammatory conditions.
Drug testing and analysis
January 1, 2012
Steven A Barker, Ethan H Mcilhenny, Rick Strassman
143 citations
Three indole alkaloids with varying psychedelic activity—DMT, bufotenine, and 5-MeO-DMT—have been reported as naturally occurring in humans. A critical review of 69 studies from 1955 to 2010 examined their detection in blood, urine, and cerebrospinal fluid. The review evaluates the methods and criteria used, highlighting strengths and weaknesses of past approaches. It notes shortcomings in existing data given recent findings and suggests future directions for research on these endogenous psychedelics.
Current drug metabolism
October 1, 2010
Hong-Wu Shen, Xi-Ling Jiang, Jerrold C Winter et al.
171 citations
5-MeO-DMT, a naturally occurring psychoactive drug, is metabolized by the enzyme CYP2D6 into the active metabolite bufotenine and is mainly inactivated by MAO-A. When taken with MAO-A inhibitors like harmaline, deamination is reduced, leading to prolonged exposure to both 5-MeO-DMT and bufotenine. These compounds act together on serotonin systems, potentially causing serotonin toxicity. CYP2D6 also metabolizes harmaline, and genetic variations in this enzyme may alter drug interactions and risks. This review covers the metabolism, pharmacokinetics, and drug-drug interactions of 5-MeO-DMT with harmaline, along with risks of intoxication.
Journal of analytical toxicology
January 1, 2005
Jason Sklerov, Barry Levine, Karla A Moore et al.
142 citations
A 25-year-old white male died after consuming herbal extracts containing beta-carbolines and hallucinogenic tryptamines. Autopsy found no anatomic cause of death. Toxicologic analysis of heart blood identified N,N-dimethyltryptamine (0.02 mg/L), 5-methoxy-N,N-dimethyltryptamine (1.88 mg/L), tetrahydroharmine (0.38 mg/L), harmaline (0.07 mg/L), and harmine (0.17 mg/L). The medical examiner ruled the cause of death as hallucinogenic amine intoxication and the manner of death as undetermined.