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首页> 外文期刊>CNS drug reviews >Neuroprotection by rasagiline: a new therapeutic approach to Parkinson's disease?
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Neuroprotection by rasagiline: a new therapeutic approach to Parkinson's disease?

机译：雷沙吉兰的神经保护作用：一种新的帕金森氏病治疗方法？

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Neuronal death in Parkinson's disease (PD) may originate from the reciprocal interactions of a restricted number of conditions, such as mitochondrial defects, oxidative stress and protein mishandling, which would favor a state of apoptotic cell death in the nigrostriatal pathway. The search for pharmacological treatments able to counteract the nigrostriatal degeneration, possibly by interfering with these phenomena, has recently raised considerable interest in rasagiline [R(+)-N-propargyl-1-aminoindan], a potent, selective, and irreversible inhibitor of monoamine oxidase B (MAO-B). Rasagiline, like selegiline, is a propargylamine, but is approximately 10 times more potent. Unlike selegiline, rasagiline is not metabolized to amphetamine and/or methamphetamine and is devoid of sympathomimetic activity. Numerous experimental studies, conducted both in vitro and in vivo, have shown that rasagiline possesses significant protective properties on neuronal populations. The pro-survival effects of the drug appear to be linked to its propargyl moiety, rather than to the inhibitory effect on MAO-B. Rasagiline's major metabolite, aminoindan - which possesses intrinsic neuroprotective activity - may also contribute to the beneficial effects of the parent compound. Rasagiline has been recently evaluated in early PD patients, with results that are consistent with slowing the progression of the disease. Therefore, the neuroprotective activity shown by the drug under experimental conditions may be reflected in the clinic, thus providing new perspectives for the treatment of PD.
机译：帕金森氏病（PD）中的神经元死亡可能源于一定数量条件的相互影响，例如线粒体缺陷，氧化应激和蛋白质处理不当，这将促进黑质纹状体途径中凋亡细胞的死亡。寻找可能通过干扰这些现象来抵消黑质纹状体变性的药物治疗方法，最近引起了对雷沙吉兰[R（+）-N-炔丙基-1-氨基茚满]的强烈兴趣，雷沙吉兰是一种有效的，选择性的且不可逆的抑制剂单胺氧化酶B（MAO-B）。雷沙吉兰与司来吉兰一样，是炔丙基胺，但效力大约是其十倍。与司来吉兰不同，雷沙吉兰不被代谢为苯丙胺和/或去氧麻黄碱，并且缺乏拟交感神经活性。在体外和体内进行的大量实验研究表明，雷沙吉兰对神经元群体具有明显的保护作用。药物的生存前作用似乎与其炔丙基部分有关，而不是对MAO-B的抑制作用有关。雷沙吉兰的主要代谢物氨基茚满-具有固有的神经保护活性-也可能有助于母体化合物的有益作用。雷沙吉兰最近已在早期PD患者中进行了评估，其结果与减慢疾病的进展相一致。因此，该药物在实验条件下表现出的神经保护活性可能会反映在临床上，从而为PD的治疗提供新的见解。

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