Class III anti-arrhythmia drug E-4031 potentiates Na+/Ca2+ exchange current in rat ventricular myocytes

被引：0
|
作者：
Wu, DM [1 ]
Lu, JY [1 ]
Wu, BW [1 ]
机构：
[1] Shanxi Med Univ, Dept Physiol, Tai Yuan 030001, Peoples R China
来源：
ACTA PHARMACOLOGICA SINICA | 2000年 / 21卷 / 03期
关键词：
E-4031; anti-arrhythmia agents; tamoxifen; tetradecanoylphorbol acetate; protein kinase C; patch-clamp techniques; sodium-calcium exchanger;
D O I：
暂无
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
AIM: To study the effects of E-4031 on the Na+/Ca2+ exchange currents (I-Na/Ca) METHODS: The quasisteady state current-voltage relationship from the isolated rat ventricular myocytes was measured using whole-cell voltage-clamp techniques with a ramp pulse protocol. RESULTS: At potential of +50 mV, E-4031 5, 10, and 20 mu mol.L-1 increased Ni2+-sensitive current from (0.48 +/- 0.12), to (0.78 +/- 0.20), (0.96 +/- 0.16), and (1.15 +/- 0.13) pA/pF, respectively; tetradecanoylphorbol acetate (TPA) 50 nmol.L-1 increased Ni2+-sensitive current from (0.60 +/- 0.16) to (1.33 +/- 0.25) pA/pF. Tamoxifen 20 mu mol.L-1 completely prevented the current changes induced by B4031 and TPA. CONCLUSION: B4031 stimulates the Na+/Ca2+ exchange via a protein kinase C-dependent pathway.
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页码：249 / 252
页数：4
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