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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268).
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Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268).

机译：新型抗胆碱酯酶抑制剂（MF268）的长效抗遗忘作用。

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摘要

In the present study a short (120 min) and long-lasting (360 min) antagonism of scopolamine-induced amnesia in rats was investigated in an eight-arm radial maze, by (3a S, 8a R)-1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-o l[8-(cis2,6-dimethyl-morpholin-4-yl)octyl]-carbamate L-bitartrate hydrate (MF268), a new cholinesterase inhibitor. Upon completing the training session, the rats were orally administered increasing doses of MF268 (2, 3, 6, 7, and 8 mg/kg) 60 min prior to s.c. injection of scopolamine (0.25 mg/kg). Following a further 60 min the rat was placed in the maze. The reversal of scopolamine-induced impairment was characterized by an inverted U-shaped dose-response curve. A significant reduction in the number of errors, and time taken to complete the maze was observed with a dose of 6 mg/kg. The compound improved memory retention without affecting scopolamine-induced hypermotility. When the same dose was administered 360 min prior to the test a significant reduction in the number of amnesic animals was observed, whereas no cognitive improvement was detected when either 1-Benzil-4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl piperidine hydrochloride (E2020) (0.25 mg/kg) or tacrine (0.5 mg/kg) were administered 360 min prior to the test. The kinetics of whole-brain cholinesterase confirmed the long-lasting activity for MF268. A clinical relevance for the use of MF268 in AD treatment is suggested.
机译：在本研究中，在八臂放射状迷宫中研究了东pol碱引起的大鼠失忆的短期（120分钟）和持久（360分钟）拮抗作用，方法为（3a S，8a R）-1,2,3 ，3a，8,8a-六氢-1,3a，8-三甲基吡咯并[2,3-b]吲哚-5-醇[8-（顺式，6-二甲基吗啉-4-基）辛基]-氨基甲酸酯L-水合酒石酸氢盐（MF268），一种新型胆碱酯酶抑制剂。在完成训练后，在皮下注射前60分钟给大鼠口服增加剂量的MF268（2、3、6、7和8 mg / kg）。注射东pol碱（0.25 mg / kg）。再过60分钟后，将大鼠置于迷宫中。东pol碱引起的损伤的逆转以倒U形剂量反应曲线为特征。剂量为6 mg / kg时，观察到错误数量和完成迷宫所需的时间大大减少。该化合物在不影响东without碱诱导的运动过快的情况下改善了记忆力。当在测试前360分钟给予相同剂量时，观察到记忆删除动物的数量显着减少，而当1-Benzil-4-[[5,6-dimethoxy-1-dandanon]中的任何一种时，均未发现认知改善。在测试前360分钟施用-2-基]-甲基哌啶盐酸盐（E2020）（0.25mg / kg）或他克林（0.5mg / kg）。全脑胆碱酯酶的动力学证实了MF268的持久活性。建议在MF治疗中使用MF268具有临床意义。

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