Characteristics of hERG and hNav1.5 channel blockade by sulcardine sulfate, a novel anti-arrhythmic compound
文献类型：期刊论文
| 作者 | Chen, Weihai1,2,3; Gan, Lu2,3; Wang, Yiping1
|
| 刊名 | European journal of pharmacology
 |
| 出版日期 | 2018-12-06 |
| 卷号 | 844页码:130-138 |
| ISSN号 | 1879-0712 |
| DOI | 10.1016/j.ejphar.2018.12.009 |
| 文献子类 | Article |
| 英文摘要 | Sulcardine sulfate (sulcardine) is a novel anti-arrhythmic compound, which blocks multiple channels and was shown to be safe and tolerated in clinical trials. The aim of the present study was to investigate the electrophysiological characteristics of sulcardine on the hERG and hNav1.5 channels. The hERG and hNav1.5 channels were heterologously stably expressed in human embryonic kidney 293 cells, and the effects of sulcardine on the hERG and hNav1.5 channels were recorded using the standard whole-cell patch-clamp technique. Sulcardine inhibited hERG channels in a concentration-dependent and reversible manner (IC = 94.3 μM). In addition, sulcardine shifted the activation curve of hERG channels to more negative potentials. The relative block of sulcardine on hERG channels was close to zero at the time point corresponding to channel opening, which was achieved by applying a depolarizing voltage, and quickly increased afterward. Sulcardine inhibited hNav1.5 channels in a concentration-dependent and reversible manner (IC = 15.0 μM) and shifted the inactivation curve of hNav1.5 channels to more negative potentials. The blockade of sulcardine on hNav1.5 channels was use-dependent. In conclusion, sulcardine is a potent hNav1.5 channel blocker with a mild inhibitory effect on hERG channels and preferentially binds to both hERG and hNav1.5 channels in the open and inactivated states rather than in the resting state. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266338]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Chen, Weihai |
| 作者单位 | 1.State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China 2.Faculty of Psychology, Southwest University, Chongqing, China; 3.Key Laboratory of Cognition and Personality (Southwest University), Ministry of Education; |
| 推荐引用方式 GB/T 7714 | Chen, Weihai,Gan, Lu,Wang, Yiping. Characteristics of hERG and hNav1.5 channel blockade by sulcardine sulfate, a novel anti-arrhythmic compound[J]. European journal of pharmacology,2018,844:130-138. |
| APA | Chen, Weihai,Gan, Lu,&Wang, Yiping.(2018).Characteristics of hERG and hNav1.5 channel blockade by sulcardine sulfate, a novel anti-arrhythmic compound.European journal of pharmacology,844,130-138. |
| MLA | Chen, Weihai,et al."Characteristics of hERG and hNav1.5 channel blockade by sulcardine sulfate, a novel anti-arrhythmic compound".European journal of pharmacology 844(2018):130-138. |
入库方式： OAI收割
来源：上海药物研究所
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