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
- 作者: Makara N.1, Sapozhnikova T.1, Khisamutdinova R.1, Tsypysheva I.1, Borisevich S.1, Kovalskaya A.1, Petrova P.1, Khursan C1, Zarudii F.1,2
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隶属关系:
- 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
- 期: 卷 164, 编号 4 (2018)
- 页面: 434-438
- 栏目: 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
如何引用文章
详细
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.
作者简介
N. Makara
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
编辑信件的主要联系方式.
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
T. Sapozhnikova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
R. Khisamutdinova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
I. Tsypysheva
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
S. Borisevich
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
A. Kovalskaya
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
P. Petrova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
C Khursan
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
俄罗斯联邦, Ufa
F. 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
俄罗斯联邦, Ufa; Ufa