In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen, N,N-[11C]dimethyltryptamine
Kazuhiko Yanai, Tatsuo Ido, Kiichi Ishiwata, Jun Hatazawa, Toshihiro Takahashi, Ren Iwata, T Matsuzawa
European Journal of Nuclear Medicine and Molecular Imaging July 1, 1986 DOI: 10.1007/bf00276707 (opens in new tab) via OpenAlex
Summary
AI-generated from the abstractThe endogenous hallucinogen N,N-dimethyltryptamine (DMT), labeled with carbon-11, accumulates preferentially in the cerebral cortex, caudate putamen, and amygdaloid nuclei of rat brain. Subcellular distribution studies show specific localization in fractions enriched with serotonin receptors only when a very low dose is injected. Pretreatment with the monoamine oxidase inhibitor pargyline greatly enhances the proportion of radioactivity in receptor-rich fractions. In dog brain, positron emission tomography demonstrates specific binding of [11C]DMT to serotonin receptors, with 5-methoxy-N,N-dimethyltryptamine causing approximately 20% displacement of the radioligand from receptors.
Study at a glance
| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Rat brain and dog brain |
| Interventions | pargyline 5-methoxy-N N-dimethyltryptamine |
| Dose | very low dose |
| Topics | Serotonin |
| Keywords | Radioligand Hallucinogen Pargyline Receptor |
| Citations | 2 |
| Key finding | DMT binds specifically to serotonin receptors, with pargyline pretreatment enhancing its localization in receptor-rich fractions and 5-methoxy-N,N-dimethyltryptamine displacing about 20% of the radioligand from receptors in dog brain. |
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.