In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen,N,N-[11C]dimethyltryptamine |
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| Authors: | Kazuhiko Yanai Tatsuo Ido Kiichi Ishiwata Jun Hatazawa Toshihiro Takahashi Ren Iwata Taiju Matsuzawa |
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| Institution: | (1) Division of Radioisotope Research, Cyclotron and Radioisotope Center, Tohoku University, 980 Sendai, Japan;(2) Department of Radiology and Nuclear Medicine, Research Institute for Tuberculosis and Cancer, Tohoku University, 980 Sendai, Japan |
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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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| Keywords: | [11C]Dimethyltryptamine Serotonin receptors Positron |
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