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.
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页码：434 / 438
页数：4
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