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[基于对各M胆碱受体亚型的选择性的毒蕈碱拮抗剂的抗帕金森病活性]

[The antiparkinson activity of muscarinic antagonists depending on their selectivity for individual m-cholinoreceptor subtypes].

作者信息

Kosmachev A B, Beliaev V A, Khrabrova A V, Fil'ko O A, Libman N M

机构信息

Laboratory of Biochemistry, Institute of Toxicology, Russian Federation Ministry of Health, St. Petersburg, Russia.

出版信息

Eksp Klin Farmakol. 1998 Sep-Oct;61(5):3-5.

PMID:9854621
Abstract

The dependence between the activity parameters of muscarine antagonists in the prevention of haloperidol catalepsy in rats and those in tests characterizing the interaction of ligands and various subtypes of m-cholinoceptors was studied. It was established by constructing the mathematical dependence that blockade of m1-cholinoceptors increases, while that of m2-cholinoceptors reduces the antiparkinsonian activity of the drugs. The activity of the muscarine antagonist pentiphan in the prevention of haloperidol-induced catalepsy in rats exceeds the activity of such traditional antiparkinsonian drugs as cyclodol and amedin.

摘要

研究了毒蕈碱拮抗剂在预防大鼠氟哌啶醇致僵方面的活性参数与在表征配体与不同亚型毒蕈碱胆碱能受体相互作用的试验中的活性参数之间的依赖性。通过构建数学相关性确定,阻断m1胆碱能受体会增强,而阻断m2胆碱能受体会降低药物的抗帕金森病活性。毒蕈碱拮抗剂喷替芬在预防大鼠氟哌啶醇诱导的僵住症方面的活性超过了环苯扎林和阿美丁等传统抗帕金森病药物的活性。

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