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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。
AIM: To investigate the effects of N- (3,5,6-trimethylpyrazine-2-formyl) -N ’- (4-fluorophenyl) piperazine (A1) on rat corpus cavernosum smooth muscle cells ) Cytoplasmic free calcium ion concentration. METHODS: Rat PCSMC were loaded with Fluo-3 / AM, a novel Ca2 + fluorescent dye. The cells were divided into KCl and NE groups, and cells were determined by laser scanning confocal microscopy (LSCM) The changes of [Ca2 +] in hippocampus were observed. The effect of different concentrations of A1 on the increase of intracellular Ca2 + concentration induced by high potassium and NE was observed and compared with that of the parental ligustrazine. Results: At rest, A1 had no significant effect on [Ca2 +] in the cytoplasm of rat PCSMC. 1, 10, 100μmol.L-1A1 could significantly inhibit the increase of intracellular calcium concentration induced by high potassium, the inhibition rates were (37.8 ± 2.3)%, (51.2 ± 3.2)% and (58.8 ± 3.0)%, respectively. (29.8 ± 3.4)%, (38.3 ± 2.5)% and (48.7 ± 3.2)%, respectively, in 1μmol.L-1NE-induced Ca2 + release from cells. CONCLUSION: The inhibitory effect of A1 on voltage-dependent calcium channel and intracellular calcium release in rat PCSMC can decrease the level of [Ca2 +] in the cytoplasm of PCSMC, and its effect is more obvious than that of ligustrazine.