季铵盐_____季铵盐；氟哌啶醇；血管平滑肌细胞；钙

N-烷基氟哌啶醇季铵盐的合成及对细胞钙离子的影响

http://www.100md.com 《广东药学院学报》 2004年第3期

季铵盐,,季铵盐；氟哌啶醇；血管平滑肌细胞；钙,1材料与方法,2结果与讨论,3结论,参考文献

     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；钙

    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

    (1.Department of Chemistry,Shantou University Medical College,Shantou,Guangdong 515041; 2.Department of Pharmacology,Shantou University Medical College,Shantou,Guangdong 515041)

    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. [Ca2+]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 Ca2+ level in the VSMCs by blocking the voltagedependent calcium channel. ......

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