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左旋多巴的“神奇之处”:为何它是帕金森病治疗的金标准?

The 'magic' of L-dopa: why is it the gold standard Parkinson's disease therapy?

作者信息

Mercuri Nicola Biagio, Bernardi Giorgio

机构信息

Clinica Neurologica Università di Roma Tor Vergata and IRCCS Fondazione Santa Lucia, Via Ardeatina 306, 00179 Roma, Italy.

出版信息

Trends Pharmacol Sci. 2005 Jul;26(7):341-4. doi: 10.1016/j.tips.2005.05.002.

DOI:10.1016/j.tips.2005.05.002
PMID:15936832
Abstract

The chronic treatment of Parkinson's disease with L-dopa is often associated with fluctuations of motor response and dyskinesias. Therefore, to overcome the adverse effects of the long-term use of L-dopa, directly acting dopamine receptor agonists have been introduced. However, L-dopa remains the most effective treatment of the slowness of movement, increased muscle tone, and tremor that are typical of Parkinson's disease. Why is this so? In this article, we discuss evidence that suggests that dopamine produced from L-dopa has a larger number of actions compared with dopamine receptor agonists. In addition to stimulating D1- and D2-like dopamine receptors, dopamine might also activate adrenoceptors, novel dopamine sites, the dopamine transporter and trace amine receptors, all of which might contribute to the superior effect of L-dopa in Parkinson's disease.

摘要

长期使用左旋多巴治疗帕金森病常伴有运动反应波动和异动症。因此,为克服长期使用左旋多巴的不良反应,已引入直接作用的多巴胺受体激动剂。然而,左旋多巴仍然是治疗帕金森病典型的运动迟缓、肌张力增高和震颤最有效的药物。为什么会这样呢?在本文中,我们讨论了相关证据,这些证据表明,与多巴胺受体激动剂相比,左旋多巴产生的多巴胺具有更多的作用。除了刺激D1样和D2样多巴胺受体外,多巴胺还可能激活肾上腺素能受体、新型多巴胺位点、多巴胺转运体和痕量胺受体,所有这些都可能有助于左旋多巴在帕金森病治疗中发挥更优疗效。

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