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

Publication date: 2018

DOI: 10.1007/s10517-018-4006-0

Abstract:

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. © 2018, Springer Science+Business Media, LLC, part of Springer Nature.

Издатель: Springer New York LLC

Тип: Article