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


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 greatly enhanced by pretreatment with the monoamine oxidase inhibitor, pargyline. Specific binding of [11C]DMT to serotonin receptors in dog brain was demonstrated by a positron emission tomographic study in which 5-methoxy-N,N-dimethyltryptamine caused approximately 20% displacement of the radioligand from the receptors.

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  1. Barker SA, Monti JA, Christian ST (1980) Metabolism of the hallucinogen N,N-dimethyltryptamine in the rat brain homogenates. Biochem Pharmacol 29:1049–1057

  2. Bennett JP, Snyder SH (1975) Stereospecific binding of d-lysergic acid diethylamide (LSD) to brain membranes: relationship to serotonin reseptors. Brain Res 94:523–544

  3. Bennett JP, Snyder SH (1976) Serotonin and lysergic acid diethylamide binding in rat brain membranes: relationship to postsynaptic serotonin receptors. Mol Pharmacol 12:373–389

  4. Berger G, Maziere M, Marazano C, Comar D (1978) Carbon-11 labeling of the psychoactive drug O-methyl-bufotenine and its distribution in the animal organism. Eur J Nucl Med 3:101–104

  5. Berridge M, Comar D, Crouzel C, Baron J-C (1982) [11C]Labeled ketanserin: a selective serotonin S2 antagonist. J Labelled Compd Radiopharmacol 20:73–78

  6. Biegon A, Rainbow TC, McEwen BS (1982) Quantitative autoradiography of serotonin receptors in the rat brain. Brain Res 242:197–204

  7. Checkley SA, Murray RM, Oon MCH, Rodnight R, Birley JLT (1980) A longitudinal study of urinary excretion of N,N-dimethyltryptamine in psychotic patients. Br J Psychiatry 137:236–239

  8. Fillion GMB, Rousselle JC, Fillion MP, Beaudoin DM, Coiny MR, Deniau JM, Jacob JJ (1977) High affinity binding of [3H]5-hydroxytryptamine to brain synaptosomal membranes: comparison with [3H]lysergic acid diethylamide binding. Mol Pharmacol 14:50–59

  9. Gillin JC, Kaplan J, Stillman R, Wyatt RJ (1976) The psychedelic model of schiophrenia: the case of N,N-dimethyltryptamine. Am J Psychiatry 133:203–208

  10. Glennon RA (1979) Serotonin receptor binding affinities of tryptamine analogues. J Med Chem 22:428–432

  11. Ishiwata K, Ido T, Monma M, Murakami M, Fukuda H, Yamada K, Endo S, Yoshioka H, Sato S, Matsuzawa T (1981) Preparation and medical application of 45Ti. Cyric Annual Report 1981, Tohoku University, (Sendai, Japan), pp 164–171

  12. Ishiwata K, Ido T, Yanai K, Kawashima K, Miura Y, Monma M, Watanuki S, Takahashi T, Iwata R (1985) Biodistribution of positron-emitting suicide inactivator of monoamine oxidase, [11C]pargyline, in mice and a rabbit. J Nucl Med 26:630–636

  13. Kloster G, Hanus J, Voges R, Stöcklin G (1984) [11C]Mesulergin, a potential agent for mapping serotonin receptor: synthesis and animal experiments. J Labelled Compd Radiopharmacol 21:1155–1156

  14. Konig FRG, Klippel RA (1967) The rat brain. A stereotaxic atlas of forebrain and lower parts of the brain stem. Robert E. Krieger. Huntington, New York

  15. Leysen JE, Niemegeers CJE, Tollenaere JP, Laduron PM (1978) Serotonergic component of neuroleptic receptors. Nature 272:168–171

  16. Narasimhachari N, Himwich HE (1973a) Gas chromatographicmass spectrometric identification of N,N-dimethyltryptamine in urine samples from drug-free chronic schizophrenic patients and its quantitation by single (selective) ion monitoring. Biochem Biophys Res Commun 55:1064–1071

  17. Narasimhachari N, Himwich HE (1973b) GC-MS identification of bufotenine in urine samples from patient with schizophrenia or infantile autism. Life Sci 12:475–478

  18. Peroutka SJ, Snyder SH (1979) Multiple serotonin receptors: Differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol binding. Mol Pharmacol 16:687–699

  19. Peroutka SJ, Lebovitz RM, Snyder SH (1981) Two distinct central serotonin receptors with different physiological functions. Science 212:827–829

  20. Sangiah S, Gomez MV, Domino EF (1979) Accumulation of N,N-dimethyltryptamine in rat brain cortical slices. Biol Psychiatry 14:925–936

  21. Takahashi T, Takahashi K, Ido T, Yanai K, Iwata R, Ishiwata K, Nozoe S (1985) [11C]Labeling of indolealkylamine alkaloids and the comparative study of their biodistributions. Int J Appl Radiat Isot 36:965–969

  22. Yanai K, Takahashi K, Ishiwata K, Takahashi T, Kawashima K, Iwata R, Ido T (1984) [11C]Labeled indolealkylamines as potential serotonin1 receptor mapping agents: Synthesis and biodistribution. J Lab Compd Radiopharm 21 (11–12):1152–1154

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Correspondence to Tatsuo Ido.

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Yanai, K., Ido, T., Ishiwata, K. et al. In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen, N,N-[11C]dimethyltryptamine. Eur J Nucl Med 12, 141–146 (1986). https://doi.org/10.1007/BF00276707

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Key words

  • [11C]Dimethyltryptamine
  • Serotonin receptors
  • Positron