HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE
Migraine and its comorbid conditions are pathogenetically associated with many factors, including hemorheological disorders. A class of drugs with a 5-HT2A antagonistic mechanism of action, is promising for the prevention and treatment of migraine attacks and concomitant pathologies.The aim of the r...
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| Format: | Article |
| Language: | Russian |
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Volgograd State Medical University, Pyatigorsk Medical and Pharmaceutical Institute
2021-03-01
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| Series: | Фармация и фармакология (Пятигорск) |
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| Online Access: | https://www.pharmpharm.ru/jour/article/view/741 |
| _version_ | 1826798961981128704 |
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| author | D. S. Yakovlev L. V. Naumenko K. T. Sultanova A. A. Spasov |
| author_facet | D. S. Yakovlev L. V. Naumenko K. T. Sultanova A. A. Spasov |
| author_sort | D. S. Yakovlev |
| collection | DOAJ |
| description | Migraine and its comorbid conditions are pathogenetically associated with many factors, including hemorheological disorders. A class of drugs with a 5-HT2A antagonistic mechanism of action, is promising for the prevention and treatment of migraine attacks and concomitant pathologies.The aim of the research is to study and compare a hemorheological activity of anti-migraine drugs, antagonists of 5-HT2A receptors of cyproheptadine, and a new drug that completed preclinical studies of the 1-(2-diethylaminoethyl)-2-(4-methoxyphenyl)-imidazo[1,2-a]benzimidazole derivative of the RU- 31 compound.Materials and methods. The study of the hemorheological activity of the RU-31 compound and cyproheptadine, was carried out using an experimental model of rabbit blood hyperthermia in vitro. Pentoxifylline was used as a reference drug. In the course of the work, the parameters of blood viscosity, aggregation and deformability of erythrocytes were recorded.Results. It has been established that in the concentration of 1 μM, the RU-31 compounds reduce blood viscosity by 17% at high shear rates, which is comparable with pentoxifylline in the concentration of 100 μM on the activity level. In the concentration of 1 μM, cyproheptadine also causes a general tendency to reduce blood viscosity at high shear rates, being inferior in activity to the RU-31 compound and pentoxifylline. In the concentration of 1 μM, the RU-31 compound has a pronounced effect on the aggregation ability of erythrocytes in autologous plasma, reducing the aggregation rate by 70%, while the level of activity is not inferior to the drug compared to pentoxifylline in the concentration of 100 μM, and surpasses the drug cyproheptadine. For the RU-31 compound and cyproheptadine, no significant effect on the deformability of erythrocytes has been shown.Conclusion. The capacity of cyproheptadine and the RU-31 compound to influence the rheological properties of blood by reducing blood viscosity and aggregation of erythrocytes has been revealed. |
| first_indexed | 2024-04-10T01:36:23Z |
| format | Article |
| id | doaj.art-e4d8e35edf7649969ac8e278b6e05626 |
| institution | Directory Open Access Journal |
| issn | 2307-9266 2413-2241 |
| language | Russian |
| last_indexed | 2025-03-14T08:59:17Z |
| publishDate | 2021-03-01 |
| publisher | Volgograd State Medical University, Pyatigorsk Medical and Pharmaceutical Institute |
| record_format | Article |
| series | Фармация и фармакология (Пятигорск) |
| spelling | doaj.art-e4d8e35edf7649969ac8e278b6e056262025-03-02T12:43:15ZrusVolgograd State Medical University, Pyatigorsk Medical and Pharmaceutical InstituteФармация и фармакология (Пятигорск)2307-92662413-22412021-03-018534535310.19163/2307-9266-2020-8-5-345-353357HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINED. S. Yakovlev0L. V. Naumenko1K. T. Sultanova2A. A. Spasov3Volgograd State Medical University; Volgograd Medical Research CenterVolgograd State Medical UniversityVolgograd State Medical University; Volgograd Medical Research CenterVolgograd State Medical University; Volgograd Medical Research CenterMigraine and its comorbid conditions are pathogenetically associated with many factors, including hemorheological disorders. A class of drugs with a 5-HT2A antagonistic mechanism of action, is promising for the prevention and treatment of migraine attacks and concomitant pathologies.The aim of the research is to study and compare a hemorheological activity of anti-migraine drugs, antagonists of 5-HT2A receptors of cyproheptadine, and a new drug that completed preclinical studies of the 1-(2-diethylaminoethyl)-2-(4-methoxyphenyl)-imidazo[1,2-a]benzimidazole derivative of the RU- 31 compound.Materials and methods. The study of the hemorheological activity of the RU-31 compound and cyproheptadine, was carried out using an experimental model of rabbit blood hyperthermia in vitro. Pentoxifylline was used as a reference drug. In the course of the work, the parameters of blood viscosity, aggregation and deformability of erythrocytes were recorded.Results. It has been established that in the concentration of 1 μM, the RU-31 compounds reduce blood viscosity by 17% at high shear rates, which is comparable with pentoxifylline in the concentration of 100 μM on the activity level. In the concentration of 1 μM, cyproheptadine also causes a general tendency to reduce blood viscosity at high shear rates, being inferior in activity to the RU-31 compound and pentoxifylline. In the concentration of 1 μM, the RU-31 compound has a pronounced effect on the aggregation ability of erythrocytes in autologous plasma, reducing the aggregation rate by 70%, while the level of activity is not inferior to the drug compared to pentoxifylline in the concentration of 100 μM, and surpasses the drug cyproheptadine. For the RU-31 compound and cyproheptadine, no significant effect on the deformability of erythrocytes has been shown.Conclusion. The capacity of cyproheptadine and the RU-31 compound to influence the rheological properties of blood by reducing blood viscosity and aggregation of erythrocytes has been revealed.https://www.pharmpharm.ru/jour/article/view/741migraine5-ht2a-antagonistshemorheologymicrocirculationdeformabilityaggregation |
| spellingShingle | D. S. Yakovlev L. V. Naumenko K. T. Sultanova A. A. Spasov HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE Фармация и фармакология (Пятигорск) migraine 5-ht2a-antagonists hemorheology microcirculation deformability aggregation |
| title | HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE |
| title_full | HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE |
| title_fullStr | HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE |
| title_full_unstemmed | HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE |
| title_short | HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE |
| title_sort | hemorheological properties of the 5 ht2a antagonist of the 2 methoxyphenyl imidazobenzimidazole derivative of the ru 31 compound and cyproheptadine in comparison with penthoxyphylline |
| topic | migraine 5-ht2a-antagonists hemorheology microcirculation deformability aggregation |
| url | https://www.pharmpharm.ru/jour/article/view/741 |
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