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[伊博格碱——结构、对人体的影响、临床意义]

[Ibogaine - structure, influence on human body, clinical relevance].

作者信息

Zdrojewicz Zygmunt, Kuszczak Bartłomiej, Olszak Natalia

机构信息

Medical University of Wrocław, Poland: 1Chair and Departament of Endocrinology, Diabetology and Izotop Therapy.

Medical University of Wrocław, Poland: Medical Faculty.

出版信息

Pol Merkur Lekarski. 2016 Jul 29;41(241):50-55.

PMID:27734823
Abstract

Ibogaine is a natural chemical compound, which belongs to the indole alkaloid family. It can be naturally found within the root bark of african plant Tabernanthe iboga. Ibogaine plays a significant role among tribal cultures. Ibogaine, in small amount, causes reduction of hunger, thirst and exhaustion. In bigger amount, however, it can cause intensive visions. Other effects include reduction or complete disappearance of absitnence symptoms visible in people addicted to the nicotine, alcohol, methamphetamine, cocaine or opioids, what has been scientifically proven after the tests on animals and small groups of people. After oral application, 80% of ibogaine is subjected to the Odemethylation into noribogaine; main catalyzing enzyme is cytochrome CYP2D6. Research suggests, that ibogaine acts in many places within central nervous system. NMDA receptors seem to play main role in its anti-addiction properties. It is important to mention the side effects of the compound, which are cardiotoxicity and neurotoxicity, what makes it harder to use its beneficial properties. Because of this, Ibogaine is included among the dangerous substance. However, there are a few clinics in the world which specializes in the use of the compound in order to interrupt the sypmtoms acute opioid withdrawal syndrome as well as a substance benficial in curing other addictions. There is more hope with synthetic derivatives of ibogaine, which although are less toxic still keep their anti-addiction properties. The aim is to collect the available knowledge related to the structure and effects on human body of alkaloid Tabernanthe iboga and consider the possibility of commercial medical use.

摘要

伊博格碱是一种天然化合物,属于吲哚生物碱家族。它天然存在于非洲植物伊博格(Tabernanthe iboga)的根皮中。伊博格碱在部落文化中起着重要作用。少量的伊博格碱会减轻饥饿、口渴和疲劳。然而,大量服用时,它会引发强烈幻觉。其他作用还包括减少或完全消除尼古丁、酒精、甲基苯丙胺、可卡因或阿片类药物成瘾者身上可见的戒断症状,这在对动物和一小群人的测试后已得到科学证实。口服后,80%的伊博格碱会通过O-去甲基化转化为去甲伊博格碱;主要催化酶是细胞色素CYP2D6。研究表明,伊博格碱在中枢神经系统的多个部位起作用。NMDA受体似乎在其抗成瘾特性中起主要作用。必须提及该化合物的副作用,即心脏毒性和神经毒性,这使得利用其有益特性变得更加困难。因此,伊博格碱被列入危险物质之列。然而,世界上有几家诊所专门使用该化合物来缓解急性阿片类药物戒断综合征的症状,以及治疗其他成瘾问题。伊博格碱的合成衍生物带来了更多希望,它们虽然毒性较小,但仍保留其抗成瘾特性。目的是收集与伊博格生物碱的结构及其对人体影响相关的现有知识,并考虑其商业医疗用途的可能性。

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1
[Ibogaine - structure, influence on human body, clinical relevance].[伊博格碱——结构、对人体的影响、临床意义]
Pol Merkur Lekarski. 2016 Jul 29;41(241):50-55.
2
How toxic is ibogaine?伊博格碱的毒性有多大?
Clin Toxicol (Phila). 2016;54(4):297-302. doi: 10.3109/15563650.2016.1138226. Epub 2016 Jan 25.
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Development of novel medications for drug addiction. The legacy of an African shrub.用于药物成瘾的新型药物的研发。一种非洲灌木的传承。
Ann N Y Acad Sci. 2000;909:88-103. doi: 10.1111/j.1749-6632.2000.tb06677.x.
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Metabolic plasticity and the energy economizing effect of ibogaine, the principal alkaloid of Tabernanthe iboga.代谢可塑性和伊博加因(Tabernanthe iboga 的主要生物碱)的能量节约效应。
J Ethnopharmacol. 2012 Aug 30;143(1):319-24. doi: 10.1016/j.jep.2012.06.039. Epub 2012 Jun 30.
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Ibogaine: complex pharmacokinetics, concerns for safety, and preliminary efficacy measures.伊波加因:复杂的药代动力学、安全性问题及初步疗效评估
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Medication development of ibogaine as a pharmacotherapy for drug dependence.作为药物依赖药物疗法的伊博格碱的药物研发。
Ann N Y Acad Sci. 1998 May 30;844:274-92.
7
Mechanisms of antiaddictive actions of ibogaine.伊博格碱的抗成瘾作用机制。
Ann N Y Acad Sci. 1998 May 30;844:214-26.
8
Ibogaine, an anti-addictive drug: pharmacology and time to go further in development. A narrative review.伊波加因,一种抗成瘾药物:药理学及进一步研发时机。一篇叙述性综述。
Hum Exp Toxicol. 2008 Mar;27(3):181-94. doi: 10.1177/0960327107087802.
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DARK Classics in Chemical Neuroscience: Ibogaine.化学生物学经典著作:伊博加因。
ACS Chem Neurosci. 2018 Oct 17;9(10):2475-2483. doi: 10.1021/acschemneuro.8b00294. Epub 2018 Oct 9.
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Ibogaine in the treatment of substance dependence.伊波加因用于物质依赖的治疗。
Curr Drug Abuse Rev. 2013 Mar;6(1):3-16. doi: 10.2174/15672050113109990001.