氨氯地平对大鼠心室肌细胞内钙离子浓度的影响

Effect of different isomers of amlodipine on cytosolic Ca^(2+) of rat ventricular myocytes

目的探讨不同旋体氨氯地平对大鼠心室肌细胞内钙离子浓度的影响。方法采用荧光探针Fura-2乙酰羧甲酯(Fura-2/AM)测定细胞内钙离子浓度,并比较1、5、10、50和100μmol/L左旋、右旋和混旋氨氯地平对细胞内钙离子浓度的影响。结果不同浓度左旋和混旋氨氯地平(1、5、10、50和100μmol/L)降低细胞内钙离子浓度分别为(1.1±0.1)%、(15.3±3.8)%、(58.1±5.2)%、(73.5±5.7)%和(88.9±7.2)%及(0.6±0.1)%、(5.1±2.0)%、(15.2±3.7)%、(65.8±4.1)%和(72.1±5.2)%;半效抑制浓度(IC50)分别为8.13)μmol/L及16.19μmol/L;不同浓度右旋氨氯地平对细胞内钙离子浓度无影响。结论左旋和混旋氨氯地平降低细胞内钙,且呈浓度依赖;而右旋氨氯地平对细胞内钙无影响。

Objective To investigate the effects of different isomers of amlodipine（Aml） on cytosolic Ca^2± of SD rat ventricular myocytes. Methods Concentrations of cytosolic Ca^2± were measured by fluorescent probe Fura-2/AM. Effects on cytosolic Ca^2± with S-Aml, R-Aml and R, S-Aml in 1,5,10,50 and 100 μmol/L were compared. Results When 1,5, 10,50 and 100 μmol/L of amlodipine were used the concentrations of cytosolic Ca^2± were reduced by （ 1.1 ± 0. 1 ） %, （ 15.3 ± 3.8） %, （58. 1 ± 5.2） %, （73.5 ± 5.7） % and （88. 9 ± 7.2） %, respectively, with a half inhibition concentration （IC50） of 8. 13 μmol/L for S-Aml, and by （0. 6 ± 0. 1） %, （5.1 ± 2.0） %, （ 15.2 ± 3. 7）%, （65.8±4. 1）% and （72.1±5.2）%, respectively, with a IC50 of 16.19 μmol/L for R, S-Aml. However, R-Aml in different concentrations had no effect on cytosolic Ca^2±. Conclusion The cytosolic Ca^2± were reduced by R, S-Aml and S-Aml, but not R-Aml.