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治疗帕金森病的多靶点药物雷沙吉兰的神经保护作用。

Neuroprotective profile of the multitarget drug rasagiline in Parkinson's disease.

机构信息

Eve Topf Centre of Excellence for Neurodegenerative Diseases and Department of Molecular Pharmacology, Technion-Rappaport Faculty of Medicine, Efron Street, P.O. Box 9697, Haifa, Israel.

出版信息

Int Rev Neurobiol. 2011;100:127-49. doi: 10.1016/B978-0-12-386467-3.00007-8.

DOI:10.1016/B978-0-12-386467-3.00007-8
PMID:21971006
Abstract

Monoamine oxidase (MAO) inhibitors were reported to have therapeutic value in several common neurodegenerative conditions owed to their diverse pharmacological functions in neuron survival. Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible MAO-B inhibitor in the treatment of Parkinson's disease (PD). It has been demonstrated to be neuroprotective in PD model systems by preventing the formation of reactive oxygen species derived from prevention of derived from oxidation of dopamine by MAO-B and via an antiapoptotic action, which appears to be independent of MAO-B inhibition and related to its embedded N-propargyl moiety. This review reflects on earlier and present evidence supporting a role for rasagiline as a neuroprotective molecule in the treatment of PD.

摘要

单胺氧化酶(MAO)抑制剂因其在神经元存活中的多种药理学功能而在几种常见的神经退行性疾病中具有治疗价值。雷沙吉兰(N-丙炔基-1-(R)-氨基茚满)是一种新型、高效的不可逆 MAO-B 抑制剂,用于治疗帕金森病(PD)。它已被证明在 PD 模型系统中具有神经保护作用,可通过防止 MAO-B 氧化多巴胺产生的活性氧的形成以及通过抗细胞凋亡作用来实现,后者似乎与 MAO-B 抑制无关,与它所嵌入的 N-丙炔基部分有关。这篇综述反映了早期和目前支持雷沙吉兰作为 PD 治疗中神经保护分子的作用的证据。

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