ru-31化合物的2-甲氧基苯基咪唑苯并咪唑衍生物和环庚啶的5- ht2a -拮抗剂与戊基茶碱的血液流变学特性比较

D. Yakovlev, L. Naumenko, K. T. Sultanova, A. Spasov
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引用次数: 3

摘要

偏头痛及其合并症在病理学上与许多因素相关,包括血液流变学疾病。一类具有5-HT2A拮抗剂作用机制的药物,有望用于预防和治疗偏头痛发作及其伴随的病理。本研究的目的是研究和比较抗偏头痛药物、赛庚啶5-HT2A受体拮抗剂和一种完成RU- 31化合物的1-(2-二乙基氨基乙基)-2-(4-甲氧基苯基)-咪唑[1,2-a]苯并咪唑衍生物临床前研究的新药的血液流变学活性。材料和方法。采用体外兔血热实验模型,研究RU-31化合物与赛庚啶的血液流变学活性。以己酮茶碱为对照药。在工作过程中,记录了血液粘度、红细胞聚集性和变形性等参数。结果表明,在1 μM浓度下,RU-31化合物在高剪切速率下可降低17%的血液粘度,其活性水平与100 μM浓度下的己酮茶碱相当。在1 μM浓度下,赛庚啶也有降低血液黏度的大趋势,其活性不如RU-31化合物和己酮茶碱。在1 μM浓度下,RU-31化合物对红细胞在自体血浆中的聚集能力有明显影响,其聚集率降低70%,而活性水平不低于100 μM浓度下的己酮茶碱,并超过药物赛庚啶。RU-31化合物和赛庚啶对红细胞的变形性无明显影响。揭示了赛庚啶和RU-31化合物通过降低血液粘度和红细胞聚集来影响血液流变学特性的能力。
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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 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.
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