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

Makara N S<sup>*</sup>; Sapozhnikova T A; Khisamutdinova R Yu; Tsypysheva I P; Borisevich S S; Kovalskaya A V; Petrova P R; Khursan C L; Zarudii F S

doi:10.1007/s10517-018-4006-0

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

作者：Makara N S^*; Sapozhnikova T A; Khisamutdinova R Yu; Tsypysheva I P; Borisevich S S; Kovalskaya A V; Petrova P R; Khursan C L; Zarudii F S

来源：Bulletin of Experimental Biology and Medicine, 2018, 164(4): 434-438.

DOI：10.1007/s10517-018-4006-0

摘要

We performed screening of nootropic properties of 10 new derivatives of quinolizidine alkaloid (-)-cytisine. Compounds with beta-endo stereochemistry were more active than alpha-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.