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CPU 86017对豚鼠心室肌细胞缓慢激活型延迟整流钾通道的抑制作用

Blocking Effect of CPU 86017 on Slowly Activated Rectifier Potassium Current in Single Ventricular Myocytes of Guinea Pigs

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【作者】 马玉萍郝雪梅张广钦周培爱吴才宏戴德哉

【Author】 MA Yu Ping, HAO Xue Mei, ZHANG Guang Qing 1, ZHOU Pei Ai, WU Cai Hong, DAI De Zai 1 Laboratory of Biological Membrane and Membrane Engineering, College of Life Science, Peking University, Beijing 100871; 1Research Division of Pharmacology, China Pharma

【机构】 北京大学生命科学院生物膜和膜生物工程实验室!北京100871中国药科大学药理学研究室!南京210009中?

【摘要】 采用全细胞膜片钳技术 ,研究 CPU860 1 7对单个豚鼠心室肌细胞延迟整流外向钾电流的缓慢激活成分 ( Iks)的作用。结果发现 CPU 860 1 7对豚鼠心室肌细胞 Iks具有电压、时间和浓度依赖性抑制作用 ( IC5 0 =1 4 .4μmol/ L)。 CPU 860 1 7使 Iks稳态激活动力学曲线倾斜 ,并明显向去极化方向移动。在用药组 ( 30μmol/ L) ,50 %最大激活电压 ( V1 / 2 )和斜率常数 ( κ)分别为 35.6± 4 .1 m V和 -1 3.7± 2 .7m V,与对照组 2 6.7± 5.1 m V和 -1 6.3± 3.9m V相比 ,P<0 .0 5。结果提示 :CPU860 1 7对单个豚鼠心室肌细胞 Iks有抑制作用

【Abstract】 Using the whole cell patch clamp technique, we studied the effects of 7 (4 chlorobenzyl) 5,8,3,13a tetrohydroberberine chloride (CPU 86017)on slowly activated outward rectifier potassium current ( I ks ) in single ventricular myocytes of guinea pigs. We found that CPU 86017 had voltage ,time and dose dependent blocking effects on I ks (IC 50 = 14.4 μmol/ L), and the steady state activation kinetics of I ks was significantly changed after the cell exposure to CPU 86017. The 50% maximal activation voltage (V 1/2 ) was 26.7±5.1 mV and 35.6± 4.1 mV in control and drug used cells, respectively ( P <0.05). The slope factor (κ)( 13.7±2.7 mV) in CPU 86017 used group was statistically changed when compared with 16.3±3.9 mV in the control ( P <0.05). The results show that CPU 86017 has blocking effects on I ks in guinea pig ventricular myocytes.

【基金】 国家自然科学基金资助项目 !(396 70 835 & 39870 883)
  • 【文献出处】 中国药科大学学报 ,JOURNAL OF CHINA PHARMACEUTICAL UNIVERSITY , 编辑部邮箱 ,2000年02期
  • 【分类号】R965
  • 【被引频次】17
  • 【下载频次】103
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