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

@article{Yanai2004InVK,
  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},
  year={2004},
  volume={12},
  pages={141-146}
}
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
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References

SHOWING 1-10 OF 23 REFERENCES
11C-labeling of indolealkylamine alkaloids and the comparative study of their tissue distributions.
TLDR
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.
TLDR
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
TLDR
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.
TLDR
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
TLDR
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.
TLDR
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
TLDR
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.
TLDR
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
...
1
2
3
...