Carvedilol Inhibits Na^+ Current in Rat Ventricular Myocytes  

作　　者：邓春玉 邝素娟 耿庆山 钱卫民 吴书林 单志新 林秋雄 杨敏 余细勇 林曙光 

机构地区：[1]Research Center of Guangdong General Hospital [2]Department of Cardiology, Guangdong Cardiovascular Institute [3]Guangdong Academy of Medical Sciences

出　　处：《South China Journal of Cardiology》2009年第2期85-89,共5页岭南心血管病杂志（英文版）

基　　金：supported by Guangdong Provincial Chinese Traditional Medicine Administration Foundation(2060033);Guangdong Provincial Medical Science and Technology Foundation (A2006002)

摘　　要：Objectives The effects of carvedilol on sodium current （INa） were investigated in isolated adult rat ventricular myocytes. Methods Single ventricular myocytes were enzymatically dissociated. INa was recorded by whole-cell patch- clamp recording technique. Results an IC50of （6. 35 - 0.40） mol . L^- 1. Carvedilol reversibly inhibited INa in a concentration-dependent manner, with 2. This inhibition was voltage- and frequency-dependent. 3. Carvedilol decreased the peak of the I-V relationship curve at -35 mV from （17.31± 1.68） pA/pF to （6. 58 ± 1.35） pA/pF, but did not change active potential, peak potential and the reverse potential significantly. 4. The steady-state inactivation curve of INa was shifted to more negative potentials. Conclusions Carvedilol inhibits INa in adult rat ventricular myocytes by mechanisms involving preferential interaction with the inactivated state of sodium channel.Objectives The effects of carvedilol on sodium current （INa） were investigated in isolated adult rat ventricular myocytes. Methods Single ventricular myocytes were enzymatically dissociated. INa was recorded by whole-cell patch- clamp recording technique. Results an IC50of （6. 35 - 0.40） mol . L^- 1. Carvedilol reversibly inhibited INa in a concentration-dependent manner, with 2. This inhibition was voltage- and frequency-dependent. 3. Carvedilol decreased the peak of the I-V relationship curve at -35 mV from （17.31± 1.68） pA/pF to （6. 58 ± 1.35） pA/pF, but did not change active potential, peak potential and the reverse potential significantly. 4. The steady-state inactivation curve of INa was shifted to more negative potentials. Conclusions Carvedilol inhibits INa in adult rat ventricular myocytes by mechanisms involving preferential interaction with the inactivated state of sodium channel.

关 键 词：CARVEDILOL whole-cell patch clamp technique sodium current （INa） rat ventricular myocytes 

分 类 号：R541[医药卫生—心血管疾病]