In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen, N,N-[11C]dimethyltryptamine

  title={In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen, N,N-[11C]dimethyltryptamine},
  author={Kazuhiko Yanai and Tatsuo Ido and Kiichi Ishiwata and Jun Hatazawa and Toshihiro Takahashi and Ren Iwata and Taiju Matsuzawa},
  journal={European Journal of Nuclear Medicine},
The endogenous hallucinogen, N,N-dimethyltryptamine (DMT), was labeled with carbon-11 and its regional distribution in rat brain studied. [11C]DMT showed higher accumulation in the cerebral cortex, caudate putamen, and amygdaloid nuclei. Studies of the subcellular distribution of [11C]DMT revealed the specific localization in the fractions enriched with serotonin receptors only when a very low dose was injected into rats. The proportions of the radioactivity in receptor-rich fractions were… 

Neuropharmacology of N,N-dimethyltryptamine

Dimethyltryptamine and other hallucinogenic tryptamines exhibit substrate behavior at the serotonin uptake transporter and the vesicle monoamine transporter

High binding-to-uptake ratios support the hypothesis that the tryptamines are transporter substrates, not uptake blockers, at both SERT and VMAT2, and indicate that there are separate substrate and inhibitor binding sites within these transporters.

Investigation of the Structure-Activity Relationships of Psilocybin Analogues.

The tryptamine derivatives have psilocybin-like pharmacological properties, supporting their classification as psychedelic drugs.

A possibly sigma-1 receptor mediated role of dimethyltryptamine in tissue protection, regeneration, and immunity

N,N-dimethyltryptamine (DMT) is classified as a naturally occurring serotonergic hallucinogen of plant origin. It has also been found in animal tissues and regarded as an endogenous trace amine

Metabolites of Tryptamine : Endogenous psychedelic neurotransmitters , and N , N dimethyltryptamine ( DMT ) in explaining a new pathway to produce Serotonin , Melatonin and hallucinations

The journey DMT takes from the intracellular makings to the sensory faking’s renown as well as new concepts to explain the chemical pathways and their associated enzymes in the brain are highlighted.

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.

Significance of mammalian N, N-dimethyltryptamine (DMT): A 60-year-old debate

Data strongly suggest that DMT can be relevant as a neurotransmitter, neuromodulators, hormone and immunomodulator, as well as being important to pregnancy and development.

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.

Dimethyltryptamine: Endogenous Role and Therapeutic Potential

While the role of endogenous DMT remains unclear, ayahuasca has promising results in anxiety, depression and substance dependence, and it is crucial to conduct further research aimed at developing new treatments for psychiatric disorders.



11C-labeling of indolealkylamine alkaloids and the comparative study of their tissue distributions.

Carbon 11 labeling of the psychoactive drug O-methyl-bufotenine and its distribution in the animal organism

A methylated derivative of serotonin, O-methyl-bufotenine has been labeled with 11C on the two methyl groups of the amine function. In order to avoid the cyclization which occurs during the

Biodistribution of a positron-emitting suicide inactivator of monoamine oxidase, carbon-11 pargyline, in mice and a rabbit.

  • K. IshiwataT. Ido R. Iwata
  • Biology, Chemistry
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine
  • 1985
The uptakes of the 11C in each organ except for the kidney and spleen seemed to correlate with the in vitro enzymatic activity of Type B MAO, and a high loading dose influenced the subcellular distribution but had little effect on tissue distribution.

Accumulation of N,N-dimethyltryptamine in rat brain cortical slices.

In general, irrespective of pharmacologic class, the tertiary amines were more potent than the secondary or primary amines, although there were some exceptions.

11C-Labeled ketanserin: A selective serotonin S2 antagonist

The product's tissue distribution in mice shows a brain uptake and cerebrum to cerebellum ratio that encourages further in vivo receptor binding studies and a ring-closure reaction in toluene of phosgene with the substituted 2-aminobenzamide precursor gives a nearly quantitative yield.

Serotonin and lysergic acid diethylamide binding in rat brain membranes: relationship to postsynaptic serotonin receptors.

The ontogeny of 5- HT and LSD binding sites is nearly identical and does not appear to depend on functionally intact presynaptic 5-HT neuronal input.

Serotonergic component of neuroleptic receptors

It is suggested that serotonergic, as well as dopamine agonists or antagonists for rat frontal cortex and striatal receptors are involved in the mechanism of action of neuroleptic drugs.

High-affinity binding of (3H) 5-hydroxytryptamine to brain synaptosomal membranes: comparison with (3H) lysergic acid diethylamide binding.

The interaction between LSD and 5- HT shows that high-affinity binding sites for 5-HT are not identical with those for LSD, since the inhibition of binding of one substance by the other is complex.