ArticleDrug metabolism and disposition: the biological fate of chemicals2011
Nonlinear pharmacokinetics of 5-methoxy-N,N-dimethyltryptamine in mice.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 27 citations in OpenAlex.
- Inhalable Psychedelic 5-MeO-DMT Shows Promise in Treatment-Resistant Depression.Journal of medicinal chemistry · 2026Article
- Short- and Long-Acting Psychedelics: Structure-Activity Relationships, Pharmacology, and Implications for Neuropsychiatric Therapeutics.ACS chemical neuroscience · 2026Review
- Trials, trips, and tribulations: pathways for implementing psychedelic therapy in Ireland.The international journal of neuropsychopharmacology · 2026Review
- Novel Thermosensitive and Mucoadhesive Nasal Hydrogel Containing 5-MeO-DMT Optimized Using Box-Behnken Experimental Design.Polymers · 2024Article
- Criticality supports cross-frequency cortical-thalamic information transfer during conscious states.eLife · 2024Article
- A Brief Review on the Potential of Psychedelics for Treating Alzheimer's Disease and Related Depression.International journal of molecular sciences · 2023Review
- A narrative synthesis of research with 5-MeO-DMT.Journal of psychopharmacology (Oxford, England) · 2022Review
- Toxicology and Analysis of Psychoactive Tryptamines.International journal of molecular sciences · 2020Review
- The epidemiology of 5-methoxy- N, N-dimethyltryptamine (5-MeO-DMT) use: Benefits, consequences, patterns of use, subjective effects, and reasons for consumption.Journal of psychopharmacology (Oxford, England) · 2018Article
- Effects of MicroRNA-34a on the Pharmacokinetics of Cytochrome P450 Probe Drugs in Mice.Drug metabolism and disposition: the biological fate of chemicals · 2017Article
- Development of a mechanism-based pharmacokinetic/pharmacodynamic model to characterize the thermoregulatory effects of serotonergic drugs in mice.Acta pharmaceutica Sinica. B · 2016Article
- Steady-state volume of distribution of two-compartment models with simultaneous linear and saturated elimination.Journal of pharmacokinetics and pharmacodynamics · 2016Article
- Behavioral and pharmacokinetic interactions between monoamine oxidase inhibitors and the hallucinogen 5-methoxy-N,N-dimethyltryptamine.Pharmacology, biochemistry, and behavior · 2016Article
- The Endogenous Hallucinogen and Trace Amine N,N-Dimethyltryptamine (DMT) Displays Potent Protective Effects against Hypoxia via Sigma-1 Receptor Activation in Human Primary iPSC-Derived Cortical Neurons and Microglia-Like Immune Cells.Frontiers in neuroscience · 2016Article
- Potentiation of 5-methoxy-N,N-dimethyltryptamine-induced hyperthermia by harmaline and the involvement of activation of 5-HT1A and 5-HT2A receptors.Neuropharmacology · 2015Article
- Interaction of psychoactive tryptamines with biogenic amine transporters and serotonin receptor subtypes.Psychopharmacology · 2014Article
- Article
- Pharmacokinetic interactions between monoamine oxidase A inhibitor harmaline and 5-methoxy-N,N-dimethyltryptamine, and the impact of CYP2D6 status.Drug metabolism and disposition: the biological fate of chemicals · 2013Article
- Genetic variability of drug-metabolizing enzymes: the dual impact on psychiatric therapy and regulation of brain function.Molecular psychiatry · 2013Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
5-Methoxy-N,N,-dimethyltryptamine (5-MeO-DMT), an abused serotonergic indolealkylamine drug, was placed into Schedule I controlled substance status in the United States as of January 19, 2011. In previous studies, we have shown the impact of monoamine oxidase A and cytochrome P450 2D6 enzymes on 5-MeO-DMT metabolism and pharmacokinetics. The aim of this study was to investigate 5-MeO-DMT pharmacokinetic properties after intravenous or intraperitoneal administration of three different doses (2, 10, and 20 mg/kg) to CYP2D6-humanized (Tg-CYP2D6) and wild-type control mice. Systemic exposure [area under the curve (AUC)] to 5-MeO-DMT was increased nonproportionally with the increase in dose. The existence of nonlinearity in serum 5-MeO-DMT pharmacokinetics was clearly manifested by dose-normalized AUC values, which were approximately 1.5- to 2.0-fold (intravenous) and 1.8- to 2.7-fold (intraperitoneal) higher in wild-type or Tg-CYP2D6 mice dosed with 10 and 20 mg/kg 5-MeO-DMT, respectively, than those in mice treated with 2 mg/kg 5-MeO-DMT. Furthermore, a two-compartment model including first-order absorption, nonlinear (Michaelis-Menten) elimination, and CYP2D6-dependent linear elimination from the central compartment was developed to characterize the intravenous and intraperitoneal pharmacokinetic data for 5-MeO-DMT in wild-type and Tg-CYP2D6 mice. In addition, 5-MeO-DMT was readily detected in mouse brain after drug treatment, and brain 5-MeO-DMT concentrations were also increased nonproportionally with the increase of dose. The results establish a nonlinear pharmacokinetic property for 5-MeO-DMT in mice, suggesting that the risk of 5-MeO-DMT intoxication may be increased nonproportionally at higher doses.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.