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_ | 1797874715840217088 |
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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 | 2024-04-10T01:36:23Z |
| 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-e4d8e35edf7649969ac8e278b6e056262023-03-13T09:18:12ZrusVolgograd 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. Spasov3Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования «Волгоградский государственный медицинский университет» Министерства здравоохранения Российской Федерации; Государственное бюджетное учреждение «Волгоградский медицинский научный центр»Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования «Волгоградский государственный медицинский университет» Министерства здравоохранения Российской ФедерацииФедеральное государственное бюджетное образовательное учреждение высшего профессионального образования «Волгоградский государственный медицинский университет» Министерства здравоохранения Российской Федерации; Государственное бюджетное учреждение «Волгоградский медицинский научный центр»Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования «Волгоградский государственный медицинский университет» Министерства здравоохранения Российской Федерации; Государственное бюджетное учреждение «Волгоградский медицинский научный центр»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.https://www.pharmpharm.ru/jour/article/view/741мигрень5-нт2а-антагонистыгемореологиямикроциркуляциядеформируемостьагрегация |
| 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) мигрень 5-нт2а-антагонисты гемореология микроциркуляция деформируемость агрегация |
| 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 | мигрень 5-нт2а-антагонисты гемореология микроциркуляция деформируемость агрегация |
| url | https://www.pharmpharm.ru/jour/article/view/741 |
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