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| 阿司咪唑阻断HERG通道的生物学特性及分子机制 | |
| 引用本文： | 涂丹娜,廖玉华,邹安若,杜以梅,肖华,王宪沛,李璐. 阿司咪唑阻断HERG通道的生物学特性及分子机制[J]. 山东医药, 2008, 48(29): 4-6 |
| 作者姓名： | 涂丹娜 廖玉华 邹安若 杜以梅 肖华 王宪沛 李璐 |
| 作者单位： | 华中科技大学同济医学院附属协和医院,湖北武汉,430022;华中科技大学同济医学院附属协和医院,湖北武汉,430022;华中科技大学同济医学院附属协和医院,湖北武汉,430022;华中科技大学同济医学院附属协和医院,湖北武汉,430022;华中科技大学同济医学院附属协和医院,湖北武汉,430022;华中科技大学同济医学院附属协和医院,湖北武汉,430022;华中科技大学同济医学院附属协和医院,湖北武汉,430022 |
| 摘 要： | 目的 观察阿司咪唑对野生型和Y652突变型HERG通道阻断的生物物理学特性,探讨HERG通道分子位点改变对阻断的影响.方法 将HERG通道表达于非洲爪蟾卵母细胞,利用双电极电压钳技术测量其电流,观察阿司咪唑不同浓度、不同电压、不同作用时间下,对野生型和Y652A、Y652R突变型HERG通道电流的阻断作用.结果 阿司咪唑以电压、浓度、时间依赖性阻断HERG通道电流;与野生型比较,Y652A和Y652R突变型可显著减弱阿司咪唑对HERG通道的阻断作用.结论 阿司咪唑优先阻断开放状态的HERG通道,Y652是阿司咪唑与通道结合的关键位点,其极性和侧链长度改变可影响阿司咪唑与通道结合. |
| 关 键 词： | HERG 钾通道 电压钳技术 阿司咪唑 突变 |
Biophysical properties and molecular mechanism of HERG channels blockade by astemizole |
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| TU Dan-na,LIAO Yu-hua,ZOU An-ruo,DU Yi-mei,XIAO Hua,WANG Xian-pei,LI Lu. Biophysical properties and molecular mechanism of HERG channels blockade by astemizole[J]. Shandong Medical Journal, 2008, 48(29): 4-6 | |
| Authors: | TU Dan-na LIAO Yu-hua ZOU An-ruo DU Yi-mei XIAO Hua WANG Xian-pei LI Lu |
| Affiliation: | The affiliated Union Hospital;Tongji Medical College of Huazhong University of Science and Technology;Wuhan 430022;P.R.China |
| Abstract: | Objective To investigate the inhibitory action of astemizole on wild type(WT) and Y652 mutational HERG channels and observe the molecular mechanism.Methods HERG channels were expressed in Xenopus oocytes,and currents were measured using two-microelectrode voltage-clamp technique.The effects of astemizole on HERG channels blockade were observed.Results Astemizole blocked HERG current in voltage-concentration-and time-dependent manner.Compared with the WT,Y652A and Y652R significantly attenuated the blockade ... |
| Keywords: | HERG |
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