氟哌啶醇季铵盐衍生物的合成及其扩冠活性的研究
Preparation of Quaternary Ammonium Salt Derivatives of Haloperidol and Their Activities on Coronary Artery
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摘要: 目的：合成氟哌啶醇季铵盐衍生物并研究其对冠状动脉的作用。方法：以氟哌啶醇为原料，将其与卤代烃在回流的情况下进行反应而得到其季铵盐衍生物。采用猪冠脉条生物测定法和Langendorff灌流法研究这些衍生物对冠状动脉的作用。结果：合成了7个新化合物(1-7)，其中化合物7量效依赖地压低KCl所致的猪冠脉条收缩曲线，阻断较大剂量所致的冠脉条痉挛，并量效依赖地拮抗脑垂体后叶素所致的离体豚鼠心脏冠脉流量减少。结论：化合物7显示了良好的扩张冠状动脉的作用，值得进一步研究。Abstract: AIM:To study the synthesis of quaternary ammonium salt derivatives of haloperidol and their effect on coronary artery METHOD S: Haloperidol was reacted with halohydrocarbon in reflux condition to synthesize the title compounds Using bioassay of porcin
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