新型磺酰胺类化合物SZ427的抗血小板聚集作用

发布时间：2018-04-09 13:44

本文选题：磺酰胺类化合物　切入点：-乙氧基-N　出处：《沈阳药科大学学报》2017年02期

【摘要】：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。
[Abstract]:Objective to study the anti-platelet aggregation effect of a new sulfonamide compound 4-ethoxy-Nu-4-pyridyl ethyl-1-3-benzenesulfonamide (SZ-427).Methods in vitro pharmacodynamics experiment, platelet aggregation analyzer was used to observe the effect of SZ427 on rabbit platelet aggregation induced by arachidonic acid, adenonisine diphosphate (ADP) and collagen.In vivo pharmacodynamics experiment, the effects of compound SZ427 on bleeding time, thrombus quality and death time were observed by three models: the bleeding time of caudal vein in mice, the common carotid artery thrombosis in rats and the acute pulmonary thrombosis in mice.Results in vitro pharmacodynamics test, compound SZ427 could significantly inhibit platelet aggregation induced by AA-ADP and collagen in rabbits, and compound SZ427 could prolong the bleeding time of tail vein and inhibit platelet aggregation in vivo.It can reduce the quality of common carotid artery thrombosis, inhibit thrombosis formation, prolong the death time of acute pulmonary thrombosis mice, and obviously reduce the death rate.Conclusion compound SZ427 can inhibit the formation of chronic and acute thrombus and has the effect of antiplatelet aggregation.
【作者单位】：沈阳药科大学生命科学与生物制药学院;
【分类号】：R96

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