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一种影响神经和行为过程的长效胆碱酯酶抑制剂。

A long-lasting cholinesterase inhibitor affecting neural and behavioral processes.

作者信息

Brufani M, Castellano C, Marta M, Oliverio A, Pagella P G, Pavone F, Pomponi M, Rugarli P L

出版信息

Pharmacol Biochem Behav. 1987 Mar;26(3):625-9. doi: 10.1016/0091-3057(87)90176-6.

Abstract

A series of analogues of physostigmine were prepared with the aim of investigating their inhibitory effects on acetylcholinesterase in the treatment of Alzheimer's disease. One of the isomers prepared was evaluated for its anticholinesterase activity in vivo, acute toxicity, and some behavioral effects. This compound was a competitive inhibitor of the enzyme and was found to antagonize the stimulating effect produced by scopolamine on locomotor activity and to facilitate memory consolidation.

摘要

为了研究毒扁豆碱类似物在治疗阿尔茨海默病中对乙酰胆碱酯酶的抑制作用,制备了一系列毒扁豆碱类似物。所制备的异构体之一被评估了其体内抗胆碱酯酶活性、急性毒性及一些行为效应。该化合物是该酶的竞争性抑制剂,并且被发现可拮抗东莨菪碱对运动活性产生的刺激作用并促进记忆巩固。

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