Nootropic Activity of a Novel (-)-Cytisine Derivative (3aR,4S,8S,12R, 12aS,12bR)-10-Methyl-2-Phenyloctahydro-1H-4,12a-Etheno-8,12-Methanopyrrolo[3’,4’:3,4]Pyrido[1,2-a] [1,5]Diazocine-1,3,5(4H)-Trione

被引：0

作者：

N. S. Makara

T. A. Sapozhnikova

R. Yu. Khisamutdinova

I. P. Tsypysheva

S. S. Borisevich

A. V. Kovalskaya

P. R. Petrova

C L. Khursan

F. S. Zarudii

机构：

[1] Russian Academy of Sciences,Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry

[2] Bashkir State Medical University,Department of Pharmacology No. 1

[3] Ministry of Health of the Russian Federation,undefined

来源：

Bulletin of Experimental Biology and Medicine | 2018年 / 164卷

关键词：

(-)-cytisine; nootropic activity; mnestic activity; molecular docking;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

We performed screening of nootropic properties of 10 new derivatives of quinolizidine alkaloid (-)-cytisine. Compounds with β-endo stereochemistry were more active than α-endo-isomers. Under stress conditions (3aR,4S,8S,12R,12aS,12bR)-10-methyl-2-phenyloctahydro-1H-4,12a-etheno-8,12-methanopyrrolo[3’,4’:3,4]pyrido[1,2-a] [1,5]diazocine-1,3,5(4H)-trione enhanced memory and had a positive effect on cognitive functions of rats. According to molecular docking data, the nootropic activity of the compound can be associated with its affinity for the glutamate-binding subunits GluK1 and GluR2 of the kainate and AMPA receptor, respectively.

引用

页码：434 / 438

页数：4

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