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胆碱酯酶抑制剂在阿尔茨海默病中的作用机制。

Mechanism of action of cholinesterase inhibitors in Alzheimer's disease.

作者信息

Håkansson L

机构信息

Department of Pharmaceutical Biosciences, Uppsala University, Sweden.

出版信息

Acta Neurol Scand Suppl. 1993;149:7-9. doi: 10.1111/j.1600-0404.1993.tb04245.x.

Abstract

Cholinesterase inhibitors, such as physostigmine and tacrine, have lately gained interest as potential drugs in the treatment of Alzheimer's disease. Already in the 1950s, it was discovered that physostigmine and tacrine were potent inhibitors of acetylcholinesterase and butyrylcholinesterase. However, later studies have shown that cholinesterase inhibitors also interact with cholinergic receptors, with sodium and potassium ion channels and effect the uptake, synthesis and release of neurotransmitters. In summary, cholinesterase inhibitors are drugs with many modes of action, which may be of advantage in the treatment of a complex disorder such as Alzheimer's disease.

摘要

胆碱酯酶抑制剂,如毒扁豆碱和他克林,近来作为治疗阿尔茨海默病的潜在药物受到关注。早在20世纪50年代,人们就发现毒扁豆碱和他克林是乙酰胆碱酯酶和丁酰胆碱酯酶的强效抑制剂。然而,后来的研究表明,胆碱酯酶抑制剂还与胆碱能受体、钠和钾离子通道相互作用,并影响神经递质的摄取、合成和释放。总之,胆碱酯酶抑制剂是具有多种作用方式的药物,这可能有利于治疗像阿尔茨海默病这样的复杂疾病。

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