Potentially hallucinogenic 5‐hydroxytryptamine receptor ligands bufotenine and dimethyltryptamine in blood and tissues

  title={Potentially hallucinogenic 5‐hydroxytryptamine receptor ligands bufotenine and dimethyltryptamine in blood and tissues},
  author={J K{\"a}rkk{\"a}inen and T Forsstr{\"o}m and Jarkko Tornaeus and Kristiina W{\"a}h{\"a}l{\"a} and Paula S. Kiuru and Aapo Honkanen and U-H. Stenman and Ursula Turpeinen and Antti Hesso},
  journal={Scandinavian Journal of Clinical and Laboratory Investigation},
  pages={189 - 199}
Bufotenine and N,N‐dimethyltryptamine (DMT) are hallucinogenic dimethylated indolethylamines (DMIAs) formed from serotonin and tryptamine by the enzyme indolethylamine N‐methyltransferase (INMT) ubiquitously present in non‐neural tissues. In mammals, endogenous bufotenine and DMT have been identified only in human urine. The DMIAs bind effectively to 5HT receptors and their administration causes a variety of autonomic effects, which may reflect their actual physiological function. Endogenous… 
Indolethylamine-N-methyltransferase Polymorphisms: Genetic and Biochemical Approaches for Study of Endogenous N,N,-dimethyltryptamine
All reported SNPs in INMT were amassed from genetic and biochemical literature and genomic databases to consolidate a blueprint for future studies aimed at elucidating whether DMT plays a physiological role.
Metabolites of Tryptamine : Endogenous psychedelic neurotransmitters , and N , N dimethyltryptamine ( DMT ) in explaining a new pathway to produce Serotonin , Melatonin and hallucinations
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Biosynthesis and Extracellular Concentrations of N,N-dimethyltryptamine (DMT) in Mammalian Brain
Results show for the first time that the rat brain is capable of synthesizing and releasing DMT at concentrations comparable to known monoamine neurotransmitters and raise the possibility that this phenomenon may occur similarly in human brains.
N, N-Dimethyltryptamine (DMT), an Endogenous Hallucinogen: Past, Present, and Future Research to Determine Its Role and Function
This report provides a historical overview of research concerning the endogenous hallucinogen N, N-dimethyltryptamine (DMT), focusing on data regarding its biosynthesis and metabolism in the brain
Neuropharmacology of N,N-dimethyltryptamine
A critical review of reports of endogenous psychedelic N, N-dimethyltryptamines in humans: 1955-2010.
A critical review of 69 published studies reporting the detection or detection and quantitation of these compounds in human body fluids addresses the methods applied and the criteria used in the determination of the presence of DMT, MDMT, and HDMT.
Dark Classics in Chemical Neuroscience: N, N-Dimethyltryptamine (DMT).
The synthesis of DMT is covered, as well as its pharmacology, metabolism, adverse effects, and potential use in medicine.
Administration of N,N-dimethyltryptamine (DMT) in psychedelic therapeutics and research and the study of endogenous DMT
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Tissue distribution, metabolism and effects of bufotenine administered to rats
Determination of potentially hallucinogenic N-dimethylated indoleamines in human urine by HPLC/ESI-MS-MS.
The bufotenine excretion of psychiatric patients was found to be higher than that of the somatic patients, and the dimethylated amines were found in significant amounts.
Rabbit Lung Indolethylamine N-Methyltransferase
Cloning and expression of a rabbit lung INMT cDNA and cloning of the rabbit INMT gene represent important steps toward determination of the function and regulation of this mammalian methyltransferase enzyme.
Urinary excretion of free bufotenin by psychiatric patients
Do classical hallucinogens act as 5-HT2 agonists or antagonists?
  • R. Glennon
  • Biology
    Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
  • 1990
A review of the existing literature suggests that where a 5-HT2 mechanism has been implicated (such as in phosphoinositide turnover, contraction of certain smooth muscle, rat-paw edema, head-twitch behavior, discriminative stimulus effects, hyperthermia, platelet aggregation, and in various other effects), the classical hallucinogens are most likely acting via an agonist, or at least via a partial agonists mechanism.
The enzymatic N-methylation of serotonin and other amines.
  • J. Axelrod
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1962
The serotonin methylating enzyme can N-methylate a variety of normally occurring compounds such as dopamine, normetanephrine, metanephine, epinephrine, tyramine, and octopamine as well as a varietyof foreign compounds suchAs ephedrine, amphetamine, aniline, normorphine,normeperidine and nornicotine.