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

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Abstract

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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References

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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

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

    Google Scholar 

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

    Google Scholar 

  • 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

    Google Scholar 

  • 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

    Google Scholar 

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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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  • DOI: https://doi.org/10.1007/BF00276707

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