艾地苯醌的化学，毒理学，药理学和药代动力学：综述。,Archives of Gerontology and Geriatrics

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艾地苯醌的化学，毒理学，药理学和药代动力学：综述。
Archives of Gerontology and Geriatrics ( IF 3.5 ) Pub Date : 1990-11-01 , DOI: 10.1016/0167-4943(90)90063-c
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Affiliation

将艾地苯醌（CV-2619）命名为化学结构为6-（10-羟基癸基）-2,3-二甲氧基-5-甲基-1,4-苯醌的合成化合物（日本商业名称：Avan ）。尽管它不溶于水，但可以使用其悬浮液并从肠中吸收得比较好。它的急性毒性非常低，在亚急性和慢性治疗中也具有良好的耐受性。到目前为止，在研究的模型中没有显示免疫原性或诱变性副作用。艾地苯醌的药理研究表明：（i）它起自由基清除剂的作用，并保护线粒体膜免于脂质过氧化；（ii）防止血小板凝集；（iii）改善由于中风或实验性脑缺血引起的血管疾病；（iv）它能恢复缺血性脑中的胆碱能和单胺能改变；（v）它改善了各种动物模型的整体脑功能（也包括记忆）。药代动力学研究已经证实，即使是口服给药，它也能到达脑细胞。根据实验数据得出的主要结论是，艾地苯醌甚至对人类与脑缺血相关的神经系统疾病也可能具有有益的作用：迄今为止，在人类临床试验中获得的结果证实了这种预期对人类脑血管疾病的有效性。

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Chemistry, toxicology, pharmacology and pharmacokinetics of idebenone: a review.

The name idebenone (CV-2619) was given to a synthetic compound the chemical structure of which is 6-(10-hydroxydecyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (commercial name in Japan: Avan). Although it is insoluble in water, suspensions of it can be applied and are absorbed relatively well from the intestine. Its acute toxicity is very low, and is well tolerated also in subacute and chronic treatments. It displayed no immunogenic or mutagenic side effects in the models studied so far. Pharmacological studies of idebenone revealed that (i) it acts as a free radical scavenger and protects the mitochondrial membrane against lipid peroxidation; (ii) it prevents platelet aggregation; (iii) it improves vascular disorders due to strokes or experimental cerebral ischemia; (iv) it recovers the cholinergic and monoaminergic changes in the ischemic brain; (v) it improves overall brain function (including memory, also) in various animal models. Pharmacokinetic studies have confirmed that it reaches the brain cells even after per os administration. The main conclusion from the experimental data was that idebenone may be of beneficial effect for the neurological disorders related to cerebral ischemia even in humans: the results obtained so far in human clinical trials confirmed the validity of this expectation for cases of human cerebrovascular disease.

更新日期：2019-11-01

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