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二乙胆碱在两种帕金森震颤动物模型中的作用。

Effects of diethylcholine in two animal models of Parkinsonism tremors.

作者信息

Matthews R T, Chiou C Y

出版信息

Eur J Pharmacol. 1979 Jun;56(1-2):159-62. doi: 10.1016/0014-2999(79)90446-1.

Abstract

(2-Hydroxyethyl) methyldiethylammonium iodide (diethylcholine; DEC) was tested against trihexyphenidyl for its ability to block tremors in two animal models of Parkinsonism tremors. Both DEC (75 mg/kg) and trihexyphenidyl (10 mg/kg) antagonized physostigmine tremors in mice. Both drugs also blocked tremors in rats which received intracaudate injections of carbachol. DEC was more efficacious than trihexyphenidyl in the rat model. No dose-related inhibition of tremors was seen for trihexyphenidyl (5--20 mg/kg) but inhibition by DEC was dose-related (25--50 mg/kg). The ED50 for tremor inhibition in the rat model by DEC was 33 mg/kg. DEC was also shown to cross the blood-brain barrier in mice. The probable mechanism of action of DEC is discussed.

摘要

对(2-羟乙基)甲基二乙铵碘化物(二乙胆碱;DEC)针对苯海索在两种帕金森震颤动物模型中阻断震颤的能力进行了测试。DEC(75毫克/千克)和苯海索(10毫克/千克)均能拮抗小鼠的毒扁豆碱震颤。两种药物还能阻断接受尾状核内注射卡巴胆碱的大鼠的震颤。在大鼠模型中,DEC比苯海索更有效。苯海索(5-20毫克/千克)未观察到与剂量相关的震颤抑制作用,但DEC的抑制作用与剂量相关(25-50毫克/千克)。DEC在大鼠模型中抑制震颤的半数有效剂量(ED50)为33毫克/千克。还显示DEC能穿过小鼠的血脑屏障。并讨论了DEC可能的作用机制。

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