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… Expand
Neuropharmacology of N,N-dimethyltryptamine
DMT appears to have limited neurotoxicity and other adverse effects except for intense cardiovascular effects when administered intravenously in large doses, and may be a useful experimental tool in exploring how the brain works and a useful clinical tool for treatment of anxiety and psychosis. Expand
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. Expand
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 amineExpand
Metabolites of Tryptamine : Endogenous psychedelic neurotransmitters , and N , N dimethyltryptamine ( DMT ) in explaining a new pathway to produce Serotonin , Melatonin and hallucinations
Why naturally occurring psychoactive psychedelics, N,N-dimethyltryptamine (DMT), 5hydroxy-DMT (Bufotenine, HDMT) and 5-Methoxy-DMT (MDMT) occur naturally in the human body has very littleExpand
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. Expand
N,N-Dimethyltryptamine attenuates spreading depolarization and restrains neurodegeneration by sigma-1 receptor activation in the ischemic rat brain
DMT may be considered as adjuvant pharmacological therapy in the management of acute cerebral ischemia and reduced the number of apoptotic and ferroptotic cells and supported astrocyte survival. Expand
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. Expand
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. Expand
Dimethyltryptamine: Possible Endogenous Ligand of the Sigma-1 Receptor?
[1] Manske RHF (1931) A synthesis of the methyltryptamines and some derivatives. Can J Res 5: 592–600 [2] Szára S (1956) Dimethyltryptamin: its metabolism in man; the relation to its psychotic effectExpand
eview europharmacology of N , N-dimethyltryptamine heresa
N,N-dimethyltryptamine (DMT) is an indole alkaloid widely found in plants and animals. It is best known for producing brief and intense psychedelic effects when ingested. Increasing evidence suggestsExpand


11C-labeling of indolealkylamine alkaloids and the comparative study of their tissue distributions.
DMT is the radiopharmaceutical of choice for the study of the serotonin action mechanism in the brain, because it has the highest radiochemical yield and the highest brain uptake of these 11C-labeled compounds. Expand
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 theExpand
Metabolism of the hallucinogen N,N-dimethyltryptamine in rat brain homogenates.
The reported extension of half-life and potentiation of DMT behavioral effects by iproniazid may be due to inhibition of NMT and DMT-NO formation rather than inhibition of monoamine oxidase. Expand
Biodistribution of a positron-emitting suicide inactivator of monoamine oxidase, carbon-11 pargyline, in mice and a rabbit.
  • K. Ishiwata, T. Ido, +6 authors R. Iwata
  • Chemistry, Medicine
  • 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. Expand
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. Expand
Stereospecific binding ofd-lysergic acid diethylamide (LSD) to brain membranes: Relationship to serotonin receptors
The evidence suggests that D-[3H]LSD binds to post-synaptic serotonin receptors, the only putative neurotransmitter with affinity for the LSD binding site, and psychotropically active alkylindoleamines are also potent displacing agents. Expand
11C-Labeled ketanserin: A selective serotonin S2 antagonist
A selective serotonin S2 receptor antagonist, ketanserin, was prepared labeled with carbon-11 by a rapid synthesis which uses no-carrier-added phosgene as the labeled precursor. The ring-closureExpand
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. Expand
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. Expand
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. Expand