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碳-11标记的致幻剂N,N-[11C]二甲基色胺的体内动力学和位移研究

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

作者信息

Yanai K, Ido T, Ishiwata K, Hatazawa J, Takahashi T, Iwata R, Matsuzawa T

出版信息

Eur J Nucl Med. 1986;12(3):141-6. doi: 10.1007/BF00276707.

DOI:10.1007/BF00276707
PMID:3489620
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.

摘要

内源性致幻剂N,N-二甲基色胺(DMT)用碳-11进行标记,并对其在大鼠脑中的区域分布进行了研究。[11C]DMT在大脑皮层、尾状壳核和杏仁核中显示出较高的蓄积。对[11C]DMT亚细胞分布的研究表明,只有在向大鼠注射极低剂量时,才会在富含5-羟色胺受体的组分中出现特异性定位。用单胺氧化酶抑制剂帕吉林预处理后,富含受体组分中的放射性比例大大提高。正电子发射断层扫描研究证实了[11C]DMT与犬脑5-羟色胺受体的特异性结合,其中5-甲氧基-N,N-二甲基色胺可使放射性配体从受体上产生约20%的位移。

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In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen, N,N-[11C]dimethyltryptamine.碳-11标记的致幻剂N,N-[11C]二甲基色胺的体内动力学和位移研究
Eur J Nucl Med. 1986;12(3):141-6. doi: 10.1007/BF00276707.
2
In vivo long-term kinetics of radiolabeled n,n-dimethyltryptamine and tryptamine.放射性标记的 n,n-二甲基色胺和色胺的体内长期动力学。
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Effects of pargyline and SKF-525A on brain N,N-dimethyltryptamine concentrations and hyperactivity in mice.帕吉林和SKF-525A对小鼠脑内N,N-二甲基色胺浓度及多动的影响。
Psychopharmacology (Berl). 1981;75(2):179-83. doi: 10.1007/BF00432184.
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In vivo metabolism of 5-methoxy-N,N-dimethyltryptamine and N,N-dimethyltryptamine in the rat.大鼠体内5-甲氧基-N,N-二甲基色胺和N,N-二甲基色胺的代谢
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6
Comparison of the brain levels of N,N-dimethyltryptamine and alpha, alpha, beta, beta-tetradeutero-N-N-dimethyltryptamine following intraperitoneal injection. The in vivo kinetic isotope effect.腹腔注射后N,N-二甲基色胺和α,α,β,β-四氘代-N,N-二甲基色胺的脑内水平比较。体内动力学同位素效应。
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The hallucinogen N,N-dimethyltryptamine (DMT) is an endogenous sigma-1 receptor regulator.致幻剂N,N-二甲基色胺(DMT)是一种内源性σ-1受体调节剂。
Science. 2009 Feb 13;323(5916):934-7. doi: 10.1126/science.1166127.

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本文引用的文献

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Two distinct central serotonin receptors with different physiological functions.两种具有不同生理功能的独特中枢5-羟色胺受体。
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Quantitative autoradiography of serotonin receptors in the rat brain.大鼠脑中5-羟色胺受体的定量放射自显影术。
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Transient Stimulation with Psychoplastogens Is Sufficient to Initiate Neuronal Growth.使用精神塑造剂进行短暂刺激足以启动神经元生长。
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Toxicokinetics and Toxicodynamics of Ayahuasca Alkaloids ,-Dimethyltryptamine (DMT), Harmine, Harmaline and Tetrahydroharmine: Clinical and Forensic Impact.死藤水生物碱、N,N-二甲基色胺(DMT)、骆驼蓬碱、骆驼蓬灵和四氢骆驼蓬碱的毒代动力学和毒效动力学:临床及法医学影响
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Indolethylamine--methyltransferase Polymorphisms: Genetic and Biochemical Approaches for Study of Endogenous ,-dimethyltryptamine.吲哚乙胺 - 甲基转移酶多态性:研究内源性N,N - 二甲基色胺的遗传和生化方法。
Front Neurosci. 2018 Apr 23;12:232. doi: 10.3389/fnins.2018.00232. eCollection 2018.
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A Model for the Application of Target-Controlled Intravenous Infusion for a Prolonged Immersive DMT Psychedelic Experience.一种用于延长沉浸式二甲基色胺迷幻体验的靶控静脉输注应用模型。
Front Pharmacol. 2016 Jul 14;7:211. doi: 10.3389/fphar.2016.00211. eCollection 2016.
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Neuropharmacology of N,N-dimethyltryptamine.N,N-二甲基色胺的神经药理学
Brain Res Bull. 2016 Sep;126(Pt 1):74-88. doi: 10.1016/j.brainresbull.2016.04.016. Epub 2016 Apr 25.
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A possibly sigma-1 receptor mediated role of dimethyltryptamine in tissue protection, regeneration, and immunity.可能与 sigma-1 受体相关的二甲色胺在组织保护、再生和免疫中的作用。
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Metabolism of the hallucinogen N,N-dimethyltryptamine in rat brain homogenates.大鼠脑匀浆中致幻剂N,N-二甲基色胺的代谢
Biochem Pharmacol. 1980 Apr 1;29(7):1049-57. doi: 10.1016/0006-2952(80)90169-0.
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Gas chromatographic-mass spectrometric identification of N:N-dimethyltryptamine in urine samples from drug-free chronic schizophrenic patients and its quantitation by the technique of single (selective) ion monitoring.无药物慢性精神分裂症患者尿液样本中N:N-二甲基色胺的气相色谱-质谱鉴定及其通过单(选择性)离子监测技术进行定量分析。
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Biodistribution of a positron-emitting suicide inactivator of monoamine oxidase, carbon-11 pargyline, in mice and a rabbit.正电子发射型单胺氧化酶自杀性失活剂碳-11帕吉林在小鼠和兔子体内的生物分布。
J Nucl Med. 1985 Jun;26(6):630-6.
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11C-labeling of indolealkylamine alkaloids and the comparative study of their tissue distributions.吲哚烷基胺生物碱的11C标记及其组织分布的比较研究。
Int J Appl Radiat Isot. 1985 Dec;36(12):965-9. doi: 10.1016/0020-708x(85)90257-1.
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Carbon 11 labeling of the psychoactive drug o-methyl-bufotenine and its distribution in the animal organism.精神活性药物邻甲基蟾毒色胺的碳-11标记及其在动物体内的分布。
Eur J Nucl Med. 1978 Apr 1;3(2):101-4. doi: 10.1007/BF00251632.
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