Open AccessHEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE
Author(s) -
D. S. Yakovlev,
Л. В. Науменко,
К.Т. Sultanova,
A. A. Spasov
Publication year - 2021
Publication title -
farmaciâ i farmakologiâ
Language(s) - English
Resource type - Journals
eISSN - 2413-2241
pISSN - 2307-9266
DOI - 10.19163/2307-9266-2020-8-5-345-353
Subject(s) - cyproheptadine , pentoxifylline , pharmacology , drug , chemistry , medicine , antagonist , receptor , serotonin
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.