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Abstract
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.
Highlights
Мигрень и ее коморбидные состояния патогенетически ассоциированы со многими факторами, в том числе и с гемореологическими нарушениями
Migraine and its comorbid conditions are pathogenetically associated with many factors, including hemorheological disorders
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
Summary
Мигрень и ее коморбидные состояния патогенетически ассоциированы со многими факторами, в том числе и с гемореологическими нарушениями. Ципрогептадин в концентрации 1 мкМ также вызывает общую тенденцию снижения вязкости крови при высоких скоростях сдвига, уступая по активности соединению РУ-31 и пентоксифиллину. Выявлена способность ципрогептадина и соединения РУ-31 оказывать влияние на реологические свойства крови путём снижения вязкости крови и агрегации эритроцитов.
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