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抗成瘾药物伊博格碱抑制人醚 - 去极化激活的钾离子通道(hERG通道):存在心律失常风险。

Anti-addiction drug ibogaine inhibits hERG channels: a cardiac arrhythmia risk.

作者信息

Koenig Xaver, Kovar Michael, Boehm Stefan, Sandtner Walter, Hilber Karlheinz

机构信息

Center for Physiology and Pharmacology, Department of Neurophysiology and - pharmacology, Medical University of Vienna, Schwarzspanierstrasse 17, 1090 Vienna, Austria.

Center for Physiology and Pharmacology, Institute of Pharmacology, Medical University of Vienna, Waehringerstrasse 13A, 1090 Vienna, Austria.

出版信息

Addict Biol. 2014 Mar;19(2):237-239. doi: 10.1111/j.1369-1600.2012.00447.x. Epub 2012 Mar 28.

DOI:10.1111/j.1369-1600.2012.00447.x
PMID:22458604
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4888945/
Abstract

Ibogaine, an alkaloid derived from the African shrub Tabernanthe iboga, has shown promising anti-addictive properties in animals. Anecdotal evidence suggests that ibogaine is also anti-addictive in humans. Thus, it alleviates drug craving and impedes relapse of drug use. Although not licensed as therapeutic drug, and despite evidence that ibogaine may disturb the rhythm of the heart, this alkaloid is currently used as an anti-addiction drug in alternative medicine. Here, we report that therapeutic concentrations of ibogaine reduce currents through human ether-a-go-go-related gene potassium channels. Thereby, we provide a mechanism by which ibogaine may generate life-threatening cardiac arrhythmias.

摘要

伊博格碱是一种从非洲灌木伊博格(Tabernanthe iboga)中提取的生物碱,已在动物实验中显示出有前景的抗成瘾特性。轶事证据表明,伊博格碱对人类也有抗成瘾作用。因此,它能减轻药物渴望并阻碍药物使用的复发。尽管未被许可作为治疗药物,且有证据表明伊博格碱可能扰乱心脏节律,但这种生物碱目前在替代医学中被用作抗成瘾药物。在此,我们报告,治疗浓度的伊博格碱会降低通过人类去极化激活的钾离子通道的电流。由此,我们提供了一种机制,通过该机制伊博格碱可能引发危及生命的心律失常。

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Long-QT syndrome induced by the antiaddiction drug ibogaine.抗成瘾药物伊博格碱诱发的长QT综合征。
N Engl J Med. 2009 Jan 15;360(3):308-9. doi: 10.1056/NEJMc0804248.
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Effects of duramycin on cardiac voltage-gated ion channels.短杆菌肽对心脏电压门控离子通道的影响。
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hERG potassium channels and cardiac arrhythmia.人醚 - 去极化激活的钾离子通道与心律失常
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Overcoming Depression with 5-HT Receptor Ligands.用 5-HT 受体配体克服抑郁症。
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Addiction. 2022 Jan;117(1):118-128. doi: 10.1111/add.15448. Epub 2021 Aug 9.
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A non-hallucinogenic psychedelic analogue with therapeutic potential.一种具有治疗潜力的非致幻性迷幻剂类似物。
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Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development.多种药物的临床前心脏电生理学、临床QT间期延长与尖端扭转型室速之间的关系:药物研发中临时安全边际的证据
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