氟哌啶醇季铵盐衍生物对血管平滑肌细胞钙离子的影响

目的　研究氟哌啶醇季铵盐衍生物 (F2 )对大鼠胸主动脉平滑肌细胞内钙离子荧光强度的影响。方法　用Ca2 +荧光染料Fluo 3 AM负载细胞 ,在激光扫描共聚焦显微镜上测定细胞内游离钙的变化。结果　在含氯化钙 (1 2 6mmol·L-1)的细胞外液中 ,30mmol·L-1KCl使细胞内钙荧光强度迅速增强 ,4种浓度F2 (0 1、1、10、10 0 μmol·L-1)作用 3min时 ,使KCl诱导细胞内钙荧光强度分别降至 6 4%± 9% ,(n=16 ,P <0 0 5 )、16 %± 5 % ,(n =2 0 ,P <0 0 1)、0 6 %±0 8% ,(n =2 0 ,P <0 0 1)、0 1%± 0 3 % ,(n =15 ,P <0 0 1) ,呈量效依赖关系。结论　F2 通过阻断细胞膜电压依赖性钙通道降低平滑肌细胞内钙浓度

Effect of quateranary ammonium salt derivative (F2) of haloperidol on calcium in vascular smooth muscle cells

AIM　To observe the effect of quateranary ammonium salt derivative (F2) of haloperidol on calcium level in vascular smooth muscle cells (VSMCs) isolated from thoracic aortas of rat. METHODS　VSMCs were loaded with Fluo-3-AM, a calcium sensitive fluorescent dye, and ［Ca2+］i was determined by the use of laser scanning confocal microscope (LCSM). RESULTS　In Ca2+ (1.26 mmol*L-1) bath solution, intracellular calcium fluorescent intensity (FI) in VSMCs was increased when application with 30 mmol*L-1 KCl, and then was inhibited after addition with F2. The FI of the ASMCs with different concentrations of F2 (0.1,1,10,100 μmmol*L-1)within three minutes were 64%±9%(n=16, P<0.05),16%±5%(n=20, P<0.01),0.6%±0.8%(n=20, P<0.01),0.1%±0.3%(n=15, P<0.01), respectively. CONCLUSION　F2 could decrease the intracellular Ca2+ level in the VSMCs by blocking the voltage-dependent calcium channel.