Email this article 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
- Authors: Makara N.S.1, Sapozhnikova T.A.1, Khisamutdinova R.Y.1, Tsypysheva I.P.1, Borisevich S.S.1, Kovalskaya A.V.1, Petrova P.R.1, Khursan CL.1, Zarudii F.S.1,2
-
Affiliations:
- Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
- Department of Pharmacology No. 1, Bashkir State Medical University, Ministry of Health of the Russian Federation
- Issue: Vol 164, No 4 (2018)
- Pages: 434-438
- Section: Pharmacology and Toxicology
- URL: https://journals.rcsi.science/0007-4888/article/view/239670
- DOI: https://doi.org/10.1007/s10517-018-4006-0
- ID: 239670
Cite item
Open Access
Access granted
Subscription Access
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.
About the authors
N. S. Makara
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Author for correspondence.
Email: newpharm@anrb.ru
Russian Federation, Ufa
T. A. Sapozhnikova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
R. Yu. Khisamutdinova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
I. P. Tsypysheva
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
S. S. Borisevich
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
A. V. Kovalskaya
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
P. R. Petrova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
C L. Khursan
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Russian Federation, Ufa
F. S. Zarudii
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences; Department of Pharmacology No. 1, Bashkir State Medical University, Ministry of Health of the Russian Federation
Email: newpharm@anrb.ru
Russian Federation, Ufa; Ufa
Supplementary files
