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

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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