The Effects of Nitroazolopyrimidines on the A1 Adenosine Receptor and Intraocular Pressure in Rats
Электронный научный архив УРФУ
Информация об архиве | Просмотр оригинала| Поле | Значение | |
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The Effects of Nitroazolopyrimidines on the A1 Adenosine Receptor and Intraocular Pressure in Rats
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| Автор |
Savateev, K. V.
Rusinov, V. L. Kotovskaya, S. K. Spasov, A. A. Naumenko, L. V. Taran, A. S. Brigadirova, A. A. Yakovlev, D. S. Sultanova, K. T. Shcherbakova, N. M. |
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| Тематика |
ADENOSINE
ADENOSINE RECEPTORS AZOLOPURINES AZOLOPYRIMIDINES GLAUCOMA INTRAOCULAR PRESSURE |
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| Описание |
Abstract: Six compounds of the 5(7)-alkylamino-6-nitroazolopyrimidine and 8-alkylazolo[5,1-b]purine series were selected based on the structural analysis of A1 adenosine receptor inhibitors and the role of this biological target in the modulation of intraocular pressure, an important factor in the pathogenesis of glaucoma. These heterocycles were shown to exhibit a weak affinity towards the A1 adenosine receptor on an in vitro model of the adenosine-dependent change of the chronotropic effect on isolated atria of white mice. On the other hand, thiadiazolo[3,2-a]pyrimidines and triazolo[5,1-b]purine displayed an in vivo hypotensive effect in rats. The leading compound, 5-methyl-8-(hydroxyethyl)triazolo[5,1-b]purine) (0.2% solution), caused a 34% reduction of ophthalmotonus in 3 h without an adverse resorptive effect. In addition, using the MTT-test it was shown on the human HepG2 cell line that the heterocycles affecting the intraocular pressure were by one to two orders of magnitude less cytotoxic than the reference doxorubicin. © 2022, The Author(s).
Ministry of Education and Science of the Russian Federation, Minobrnauka, (075-15-2020-777) The work was supported by the Ministry of Science and Higher Education of the Russian Federation, project no. 075-15-2020-777. |
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| Дата |
2024-04-08T11:07:25Z
2024-04-08T11:07:25Z 2022 |
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| Тип |
Article
Journal article (info:eu-repo/semantics/article) Published version (info:eu-repo/semantics/publishedVersion) |
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| Идентификатор |
Savateev, KV, Rusinov, VL, Kotovskaya, SK, Spasov, AA, Naumenko, LV, Taran, AS, Brigadirova, AA, Yakovlev, DS, Sultanova, KT & Shcherbakova, NM 2022, 'The Effects of Nitroazolopyrimidines on the A1 Adenosine Receptor and Intraocular Pressure in Rats', Russian Journal of Bioorganic Chemistry, Том. 48, № 4, стр. 777-782. https://doi.org/10.1134/S1068162022040185
Savateev, K. V., Rusinov, V. L., Kotovskaya, S. K., Spasov, A. A., Naumenko, L. V., Taran, A. S., Brigadirova, A. A., Yakovlev, D. S., Sultanova, K. T., & Shcherbakova, N. M. (2022). The Effects of Nitroazolopyrimidines on the A1 Adenosine Receptor and Intraocular Pressure in Rats. Russian Journal of Bioorganic Chemistry, 48(4), 777-782. https://doi.org/10.1134/S1068162022040185 1068-1620 Final All Open Access; Hybrid Gold Open Access https://link.springer.com/content/pdf/10.1134/S1068162022040185.pdf https://link.springer.com/content/pdf/10.1134/S1068162022040185.pdf http://elar.urfu.ru/handle/10995/131451 10.1134/S1068162022040185 85138510434 000853071000009 |
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| Язык |
en
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| Права |
Open access (info:eu-repo/semantics/openAccess)
cc-by https://creativecommons.org/licenses/by/4.0/ |
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| Формат |
application/pdf
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| Издатель |
Pleiades Publishing
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| Источник |
Russian Journal of Bioorganic Chemistry
Russian Journal of Bioorganic Chemistry |
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