氟哌啶醇季铵盐衍生物的合成及其扩冠活性的研究(英文)  

Preparation of Quaternary Ammonium Salt Derivatives of Haloperidol and Their Activities on Coronary Artery

作　　者：郑锦鸿[1] 石刚刚[2] 盘鹰[1] 李长潮[1] 

机构地区：[1]汕头大学医学院化学教研室,汕头515031 [2]汕头大学医学院药理学教研室,汕头515031

出　　处：《中国药科大学学报》2003年第6期487-490,共4页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目 (No .30 0 70 30 4 ) ;国家新药基金资助项目 (No .96 90 1 0 52 3);中华人民共和国教育部及广东省博士基金资助项目 (No 974 2 1 6 )~~

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 。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 porcine coronary artery and Langendorff perfusion tested the effects of these compounds on coronary artery RES U LTS:Seven new quaternary ammonium salt derivatives (1-7 ) wer e synthesized Compound 7 was shown to d ecrease the contraction curve of coronary artery strips induced by KCl in dose- d ependent manner and block the contraction induced by KCl Compound 7 was found to antagonize the reduction of coronary flow induced by pituitrin on isolated heart of guinea-pig in dose-dependent manner CONCLUSION : compound 7 showed ideal and potential effect on coronary artery, and is wo rthy for further study

关 键 词：合成 季铵盐 氟哌啶醇 冠状动脉 

分 类 号：R914[医药卫生—药物化学]