氟哌啶醇季铵盐衍生物的合成及其对冠状动脉的作用  

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

作　　者：郑锦鸿[1] 石刚刚[2] 盘鹰[1] 李长潮[2] 

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

出　　处：《汕头大学医学院学报》2002年第1期11-13,共3页Journal of Shantou University Medical College

基　　金：教育部留学回国人员科研启动基金课题 ;国家自然科学基金立项课题 ( 30 0 70 30 4) ;广东省博士科研启动基金课题( 9742 16) ;广东省科技计划项目 (C30 10 4)

摘　　要：目的 :合成氟哌啶醇季铵盐衍生物并研究其对动物冠状动脉的作用。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。采用猪冠状动脉条生物测定法和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所致的猪冠状动脉条收缩曲线 ,阻断较大剂量所致的冠状动脉条痉挛 ,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 。Objective: To study the synthesis and the effect on coronary artery of quaternary ammonium salt derivatives. Methods: Haloperidol was reacted with halohydrocarbon in reflux condition to synthesize the title compounds.Bioassay of porcine coronary artery and Langendorff perfusion were used to test the effects of these compounds on coronary artery. Results:Seven quaternary ammonium salt derivatives(1～7)were synthesized. They were new compounds. Compound 7 decreased coronary artery strips contraction curve induced by KCl in dose dependent manner and blocked the contraction induced by KCl. Compound 7 also antagonized the reduction of coronary flow induced by pituitrin on isolated heart of gui nea pig in dose dependent manner. Conclusion: compound 7 shows the ideal and potential effect on coronary artery, and is worth further studying.

关 键 词：合成 季铵盐 氟哌啶醇 冠状动脉 

分 类 号：R971.4[医药卫生—药品] TQ463.54[医药卫生—药学]