CAJ | 학술논문

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.
목적:합성불고정순계안염연생물병연구기대관상동맥적작용.방법:이불고정순위원료,장기여서대경재회류적정황하진행반응이득도기계안염연생물.채용저관맥조생물측정법화Langendorff관류법연구저사연생물대관상동맥적작용.결과:합성료7개신화합물(1-7),기중화합물7량효의뢰지압저KCl소치적저관맥조수축곡선,조단교대제량소치적관맥조경련,병량효의뢰지길항뇌수체후협소소치적리체돈서심장관맥류량감소.결론:화합물7현시료량호적확장관상동맥적작용,치득진일보연구.
AIM:To study the synthesis of quaternary ammonium salt derivatives of haloperidol and their effect on coronary artery. METHODS: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. RESULTS:Seven new quaternary ammonium salt derivatives (1-7) were synthesized. Compound 7 was shown to decrease the contraction curve of coronary artery strips induced by KCl in dose-dependent 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 worthy for further study.