Tissue distribution, metabolism and effects of bufotenine administered to rats

  title={Tissue distribution, metabolism and effects of bufotenine administered to rats},
  author={Ray W. Fuller and Harold D. Snoddy and Kenneth W. Perry},

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

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.

Metabolism and urinary disposition of N,N-dimethyltryptamine after oral and smoked administration: a comparative study.

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

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

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.

Metabolism and disposition of N,N-dimethyltryptamine and harmala alkaloids after oral administration of ayahuasca.

The present results show the existence in humans of alternative metabolic routes for DMT other than biotransformation by MAO and that O-demethylation plus conjugation is an important but probably not the only metabolic route for the harmala alkaloids in humans.

Indolealkylamines: Biotransformations and Potential Drug–Drug Interactions

  • A. Yu
  • Biology
    The AAPS Journal
  • 2008
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.

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.

Recreational Use, Analysis and Toxicity of Tryptamines

Information from Internet and from published scientific literature, organized in the way proposed in this review, provides an effective tool for specialists facing the emerging NPS threat to public health and public security, including the personnel working in Emergency Department.



Distribution, metabolism and excretion of bufotenine in the rat with preliminary studies of its O-methyl derivative.

  • E. SandersM. T. Bush
  • Chemistry, Biology
    The Journal of pharmacology and experimental therapeutics
  • 1967
Studies of the biologic fate of bufoatenine and O-methyl-bufo-tenine in the rat are presented. The syntheses of these compounds labeled with C 14 and methods for estimation of unchanged compounds and

Serotonin receptor subtypes involved in the elevation of serum corticosterone concentration in rats by direct- and indirect-acting serotonin agonists.

The serum corticosterone concentration in rats was increased by injection of quipazine, a relatively nonselective serotonin agonist, or 8-hydroxy-2-(di-n- propylamino)tetralin (8-OH-DPAT), a serotonin agonists selective for the 5-HT1A subtype of receptor.

The effects of metergoline and other serotonin receptor antagonists on serum corticosterone in rats.

Metergoline antagonized the elevation of serum corticosterone by quipazine in rats and may have occurred at receptors that are not serotonin receptors or that represent a subset of serotonin receptors not mediating the actions of serotoninergic agents other than quipazines.

Role of type A and Type B MAO in the metabolism of epinephrine in rat brain

Three different catecholamines appear to be neurotrans-mitters in brain: dopamine, norepinephrine and epinephrine, which are extensively studied as brain neurotransmitters during the past two decades.

Serotonergic stimulation of pituitary-adrenocortical function in rats.

  • R. Fuller
  • Biology, Medicine
  • 1981
Various pharmacologic studies have supported a stimulatory role of brain serotonin neurons in the hypothalamic regulation of pituitary-adrenocortical function in rats. The serotonin precursor L-5-hydr

Misuse and legend in the "toad licking" phenomenon.

  • T. Lyttle
  • Political Science
    The International journal of the addictions
  • 1993
The uses of bufo toad secretions have occurred throughout history in a variety of cultural milieus and are explored as a backdrop to contemporary drug use/misuse issues.

Function and Regulation of Monoamine Enzymes: Basic and Clinical Aspects

The administration of various neuroleptic drugs results in the activation of retinal tyrosine hydroxylase of dark adapted rats. Kinetic analysis reveals that activation is due to a decrease of the Km