Tissue distribution, metabolism and effects of bufotenine administered to rats

@article{Fuller1995TissueDM,
  title={Tissue distribution, metabolism and effects of bufotenine administered to rats},
  author={Ray W. Fuller and Harold D. Snoddy and Kenneth W. Perry},
  journal={Neuropharmacology},
  year={1995},
  volume={34},
  pages={799-804}
}

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

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A new finding was the detection of large amounts of bufotenine in stools, which may be an indication of its role in intestinal function, and only small amounts of the DMIAs were found in somatic or neural tissues and none in blood.

Psychedelic 5-methoxy-N,N-dimethyltryptamine: metabolism, pharmacokinetics, drug interactions, and pharmacological actions.

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Findings show that in the smoked route a shift from the highly efficient MAO-dependent to the less efficient CYP-dependent metabolism takes place, which leads to psychoactivity and is analogous to that observed in ayahuasca preparations combining DMT with MAO inhibitors.

Biological Effects and Biodistribution of Bufotenine on Mice

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Results show that the effective dose, 0.63 mg/day, is safe to be administered in mice, since it did not cause significant effects on the animals' physiology and on the CNS, and higher doses were well tolerated.

Bufotenine: Toward an Understanding of Possible Psychoactive Mechanisms

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Support is shown for the rationale that the reported lack of the drug's classic hallucinogenic response in human experiments is due to poor ability to cross the blood brain barrier (BBB), not lack of activation of the appropriate brain receptors.

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This LC-MS/MS method is a sensitive and reliable assay for quantitation of blood 5-MeO-DMT and bufotenine and may significantly contribute to the apparent pharmacological and toxicological effects of 5-Methoxy-N,N-dimethyltryptamine.

Indolealkylamines: Biotransformations and Potential Drug–Drug Interactions

  • A. Yu
  • Biology
    The AAPS Journal
  • 2008
TLDR
An important role for polymorphic cytochrome P450 2D6 (CYP2D 6) in the metabolism of IAA drugs of abuse has been revealed by recent studies, suggesting that variations in IAA metabolism, pharmaco- or toxicokinetics and dynamics can arise from distinct CYP2D6 status, and CYP1D6 polymorphism may represent an additional risk factor in the use of these IAAdrugs.

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