N-(3,5,6-三甲基吡嗪-2-甲酰基)-N′-(4-氟基苯基)哌嗪对平滑肌细胞游离钙浓度的影响  

Effect of N-(3,5,6-trimethylpyrazine-2-methenyl)-N'-(4-fluorophenyl)piperazine on cytosolic free calcium concentration in smooth muscle cells in rat

作　　者：尹春萍[1] 张立冬[1] 刘继红[2] 刘妙娜[1] 林智成[1] 严书超[1] 

机构地区：[1]华中科技大学同济医学院药学院天然药物化学与资源评价湖北省重点实验室,湖北武汉430014 [2]华中科技大学同济医院,湖北武汉430030

出　　处：《中国医院药学杂志》2009年第15期1264-1267,共4页Chinese Journal of Hospital Pharmacy

基　　金：湖北省科技攻关项目(编号:2007AA301B26-1)

摘　　要：目的:研究N-(3,5,6-三甲基吡嗪-2-甲酰基)-N′-(4-氟基苯基)哌嗪(A1)对大鼠阴茎海绵体平滑肌细胞(PCSMC)胞质内游离钙离子浓度的影响。方法:用新型Ca2+荧光染色剂Fluo-3/AM负载大鼠PCSMC,细胞分为氯化钾(KCl)和去甲肾上腺素(NE)作用组,应用激光扫描共聚焦显微镜(LSCM)实时测定胞质内[Ca2+]的变化,分别观察不同浓度的A1对高钾和NE诱导胞质内钙浓度升高的影响,并与母药川芎嗪作用相比。结果:静息状态下,A1对大鼠PCSMC胞质内[Ca2+]无明显影响。1,10,100μmol.L-1A1能显著抑制高钾诱发的细胞内的钙浓度升高的影响,抑制率分别为(37.8±2.3)%,(51.2±3.2)%和(58.8±3.0)%。也能抑制1μmol.L-1NE诱发钙库释放的细胞内[Ca2+]升高,抑制率分别为(29.8±3.4)%,(38.3±2.5)%和(48.7±3.2)%。结论:A1对大鼠PCSMC电压依赖性钙通道和细胞内钙库释放的抑制作用,能降低PCSMC胞质内[Ca2+]水平,其作用效果比母药川芎嗪明显。OBJEcTIVE To study the effects of A1 on intracellular free calcium[Ca^2＋]in cultured penis corpus cavernosum smooth muscle cells （PCSMC） in Rat. METHODS By using laser scanning confocal microscope（LSCM）, the[Ca^2＋]i Chinge of fluorescence signal was investigated in cultured PCSMC loaded with Ca^2＋ indicator Fluo-3/AM. Compared with TMP, the effect of AI was observed in different concentrations on [Ca^2＋]i increase induced by high potassium and NE. RESULTS A1 had no obvious effect on resting PCSMC [Ca^2＋]i, It was found that 1,10,100μmol·L^-1 A1 significantly inhibited [Ca^2＋]i increase induced by high potassium depolarization. The peak inhibition rates were （37. 8±2. 3）%, （51.2±3. 2）% and （58. 8±3. 0）% respectively. A1 could also inhibit cytosolic calcium pool release induced by μmol·L^-1 NE. The peak inhibition rates were （29. 8±3. 4）%, （38. 3±2. 5） % and （48. 7±3. 2）% respectively. CONCLUSION A1 can inhibit rat PCSMC [Ca^2＋]i significantly by suppressing voltage dependent calcium channel and eytosolie calcium pool release. Compared with TMP, its effect was better.

关 键 词：川芎嗪衍生物(A1) 平滑肌细胞 激光扫描共聚焦显微镜 钙通道 

分 类 号：R963[医药卫生—微生物与生化药学]