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N-烷基氟哌啶醇季铵盐的合成及对细胞钙离子的影响
引用本文:郑锦鸿,石刚刚,盘鹰,韦日升.N-烷基氟哌啶醇季铵盐的合成及对细胞钙离子的影响[J].广东药学院学报,2004,20(3):209-211.
作者姓名:郑锦鸿  石刚刚  盘鹰  韦日升
作者单位:汕头大学医学院,化学教研室,广东,汕头,515041;汕头大学医学院,药理教研室,广东,汕头,515041
基金项目:教育部留学回国人员科研启动基金课题,广东省自然科学基金立项课题 (No .0 346 14 ),2 0 0 2年广东省教育厅“千百十工程”优秀人才培养基金 (校级 )
摘    要:目的:合成N-烷基氟哌啶醇季铵盐衍生物并研究其对血管平滑肌细胞钙离子的作用。方法:以氟哌啶醇为原料,将其与碘代烷在回流的情况下进行反应而得到相应季铵盐衍生物。以激光扫描共聚焦显微镜技术测定活细胞内钙离子的动态变化。结果:合成了6个新化合物(Ⅰ—Ⅵ),其中化合物Ⅳ量效依赖地使KCl诱导的细胞内钙荧光强度出现持续性下降。结论:Ⅳ具有抑制KCl诱导的血管平滑肌细胞电压信赖性钙通道的开放作用,从而降低细胞内的钙离子浓度。

关 键 词:季铵盐  氟哌啶醇  血管平滑肌细胞  
文章编号:1006-8783(2004)03-0209-03
修稿时间:2004年4月12日

Preparation of N-alkyl quaternary ammonium salt derivatives of haloperidol and their effects on calcium
ZHENG Jin-hong ,SHI Gang-gang ,PAN Yin ,WEI Ri-sheng.Preparation of N-alkyl quaternary ammonium salt derivatives of haloperidol and their effects on calcium[J].Academic Journal of Guangdong College of Pharmacy,2004,20(3):209-211.
Authors:ZHENG Jin-hong  SHI Gang-gang  PAN Yin  WEI Ri-sheng
Institution:ZHENG Jin-hong 1,SHI Gang-gang 2,PAN Yin 1,WEI Ri-sheng 2
Abstract:Objective: To study the synthesis of N-alkyl quaternary ammonium salt derivatives of haloperidol and their effect on calcium in vascular smooth muscle cells. Methods: Haloperidol is reacted with alkyl iodide in reflux condition to synthesize the title compounds I-VI. Ca 2+] i was determined by the use of laser scanning confocal microscope (LCSM). Results: Six N-alkyl quaternary ammonium salt derivatives (I-VI) were synthesized. They are new compounds. Compound IV decreased intracellular calcium fluorescent intensity (FI) in VSMCs induced by KCl in dose-dependent manner. Conclusion: Compound IV could decrease the intracellular Ca 2+ level in the VSMCs by blocking the voltage-dependent calcium channel.
Keywords:quaternary ammonium salt  haloperidol  vascular smooth muscle cells  calcium
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