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目的研究新型磺酰胺类化合物4-乙氧基-N,N’-二(4-吡啶乙基)-1,3-苯二磺酰胺(SZ427)的抗血小板聚集作用。方法在体外药效学实验中,采用血小板聚集分析仪观察化合物SZ427对花生四烯酸(arachidonic acid,AA)、二磷酸腺苷(adenonisine disphosphate,ADP)和胶原诱导的家兔血小板聚集的影响。在体内药效学实验中,通过小鼠尾静脉出血时间、大鼠颈总动脉血栓和小鼠急性肺血栓三种模型分别观察化合物SZ427对出血时间、血栓质量和死亡时间的影响。结果在体外药效实验中,化合物SZ427能显著抑制AA、ADP和胶原诱导的家兔血小板的聚集作用;在体内药效学实验中,化合物SZ427能延长小鼠尾静脉出血时间,具有抗血小板聚集作用;能减少大鼠颈总动脉血栓质量,抑制血栓形成;能显著延长急性肺血栓小鼠的死亡时间,明显降低死亡率。结论化合物SZ427能抑制慢性血栓和急性血栓的形成,具有抗血小板聚集的作用。
Objective To study the antiplatelet aggregation effect of a novel sulfonamide compound 4-ethoxy-N, N’-bis (4-pyridylethyl) -1,3-benzene disulfonamide (SZ427). Methods In vitro pharmacodynamic experiments, the platelet aggregation analyzer was used to observe the effect of compound SZ427 on platelet aggregation induced by arachidonic acid (AA), adenosine diphosphate (ADP) and collagen in rabbits. In vivo pharmacodynamics experiments, the impact of compound SZ427 on bleeding time, thrombus quality and death time were observed by three kinds of models: tail vein bleeding time, carotid artery thrombosis in rats and acute pulmonary thrombus in mice. Results Compound SZ427 significantly inhibited platelet aggregation induced by AA, ADP and collagen in vitro. In vivo pharmacodynamics, compound SZ427 prolonged the bleeding time of tail vein in mice and possessed antiplatelet aggregation Can reduce the thrombus quality of the common carotid artery in rats and inhibit the thrombosis; can significantly prolong the death time of acute pulmonary thrombosis mice, significantly reduce the mortality rate. Conclusion Compound SZ427 can inhibit the formation of chronic thrombus and acute thrombus and has the effect of anti-platelet aggregation.