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乌头碱对表达在卵母细胞上的hKv1.5通道的阻断作用
引用本文:李宜富,廖玉华,涂丹娜,肖华,董少红.乌头碱对表达在卵母细胞上的hKv1.5通道的阻断作用[J].中国心脏起搏与心电生理杂志,2010,24(2):167-171.
作者姓名:李宜富  廖玉华  涂丹娜  肖华  董少红
作者单位:1. 华中科技大学同济医学院附属协和医院离子通道病研究中心心内科,心血管病研究所,湖北武汉,430022
2. 暨南大学第二临床医学院,深圳市人民医院,心内科,广东深圳,518020
摘    要:目的观察乌头碱对表达在卵母细胞上的hKv1.5电流的影响。方法 hKv1.5通道表达在非洲爪蟾卵母细胞上,利用双电极电压钳技术测量其电流。结果①hKv1.5通道可以稳定表达在卵母细胞上;②乌头碱以浓度和电压依赖性方式阻断表达在卵母细胞上的hKv1.5通道,阻断的IC50值是0.796±0.123μmol/L,其Hill系数为0.280±0.020;③乌头碱对hKv1.5电流的阻断呈时间和频率依赖性。结论乌头碱对hKv1.5电流呈浓度、电压和时间依赖性阻断,提示乌头碱可能是一种开放型钾通道阻断剂,它对开放状态和失活状态下的hKv1.5通道均具有阻断作用。

关 键 词:电生理学  乌头碱  hKv1.5  心律失常  钾通道  电压钳技术

Electropharmacological properties of aconitine blocks on hKv1.5 potassium channels expressed on Xenopus laevis oocytes
LI Yi-fu,LIAO Yu-hua,TU Dan-na,XIAO Hua,DONG Shao-hong.Electropharmacological properties of aconitine blocks on hKv1.5 potassium channels expressed on Xenopus laevis oocytes[J].Chinese Journal of Cardiac Pacing and Electrophysiology,2010,24(2):167-171.
Authors:LI Yi-fu  LIAO Yu-hua  TU Dan-na  XIAO Hua  DONG Shao-hong
Institution:1 Research Center of Ion Channelopathy, Department of Cardiology, Institute of Cardiovachlar Disease, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China; 2 The Second Clinical Medical College of Jinan University ( Shenzhen Peoples Hospital) ,Shenzhen 518020 ,Guangzhou ,China)
Abstract:Objective To investigate the inhibitory action of aconitine on human Kvl. 5 ( hKv1. 5) channels expressed on Xenopus laevis oocytes. Methods hKv1. 5 channels were expressed on Xenopus laevis oocytes and studied using two microelectrode voltage clamp technique. Results HKv1. 5 channels could be stably expressed on Xenopus laevis oocytes. Aconitine produced a voltage- and time-dependent inhibition on hKvl. 5 channels expressed on Xenopus laevis oocytes. Meanwhile, the inhibition on hKvl. 5 channels was concentrition-dependent. The IC50 and Hill coefficient were 0. 796 +0. 123 μmol/L and 0.280 ±0.020 respectively, and this action could be partly reversable . On the other hand, the suppresion action was frequncy-dependent. Conclusions Aconitine blocks hKvl. 5 channel in a voltage-and time-and concentration-and frequncy-dependent fasion, futhermore, it inhibits the channels either in open or in inactive state. So it indicates that aonnitine may be an open state inhibiter of hKv1. 5 potassium channels. Chinese Journal of Cardiac Pacing and Electrophysiology, 2010,24 (2) : 167 - 171 ]
Keywords:Electrophysiology  Acontine  Human KV1  5  Arrhythmias  Potassium channels  Voltage clamp technique
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