Отправить статью по E-mail 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
- Авторы: 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
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Учреждения:
- 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
- Выпуск: Том 164, № 4 (2018)
- Страницы: 434-438
- Раздел: Pharmacology and Toxicology
- URL: https://journal-vniispk.ru/0007-4888/article/view/239670
- DOI: https://doi.org/10.1007/s10517-018-4006-0
- ID: 239670
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Аннотация
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.
Об авторах
N. Makara
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Автор, ответственный за переписку.
Email: newpharm@anrb.ru
Россия, Ufa
T. Sapozhnikova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, Ufa
R. Khisamutdinova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, Ufa
I. Tsypysheva
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, Ufa
S. Borisevich
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, Ufa
A. Kovalskaya
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, Ufa
P. Petrova
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, Ufa
C Khursan
Laboratory of Bioorganic Chemistry and Catalysis, Ufa Institute of Chemistry, Russian Academy of Sciences
Email: newpharm@anrb.ru
Россия, 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
Россия, Ufa; Ufa
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