Effects of the gastrointestinal prokinetic agent cisapride on human ether-a-go-go related gene 2 channels expressed on HEK293 cells

doi:10.3969/j.issn.1006-7795.2014.06.016

Journal of Capital Medical University ›› 2014, Vol. 35 ›› Issue (6): 760-764.doi: 10.3969/j.issn.1006-7795.2014.06.016

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Effects of the gastrointestinal prokinetic agent cisapride on human ether-a-go-go related gene 2 channels expressed on HEK293 cells

Yuan Shasha^1,2, Huang Haixia^3,4, Yang Jinkui^1,2

1. Department of Endocrine and Metabolic Diseases, Beijing Tongren Hospital, Capital Medical University, Beijing 100730, China;
2. Beijing Key Laboratory of Diabetes Research and Care Beijing 100730, China;
3. Department of Physiology and Pathophysiology, School of Basic Medical Sciences, Capital Medical University, Beijing 100069, China;
4. Beijing Key Laboratory of Metabolic Disorders Related Cardiovascular Diseases, Capital Medical University, Beijing 100069, China

Received:2014-11-06 Published:2014-12-15
Supported by:
This study was supported by National Natural Science Foundation of China(81471014, 81270918); Natural Science Foundation of Beijing(7131005).

Abstract

Abstract:

Objective To study the effects of the gastrointestinal prokinetic agent cisapride on human ether-a-go-go related gene 2(hERG2) channels expressed on HEK293 cells. Methods hERG2 cDNA(Gene Bank accession number AF311913) was transfected transiently into the HEK293 cells using Lipofectamine 2000. HERG2 current was recorded by a whole-cell patch clamp technique before and after disposal of cisapride(0.001, 0.01, 0.1, 1.0 and 10.0 μmol/L) at the time of 2, 4, 6 and 8 min. Results The amplitude of steady-state current and peak-tail current was reduced at different cisapride concentrations. The blockage of hERG2 by cisapride is strengthened with the increasing of drug concentration at the depolarization voltage of +20 mV. The effect of cisapride is also strengthened with time, and the hERG2 current vanished at the time of 8 min with 1 μmol/L cisapride. Conclusion Cisapride blocked the hERG2 channel expressed on the HEK293 cells, including the step current and tail current. The blocking of hERG2 by cisapride is concentration dependent and time dependent simultaneously until the tail current was reduced to steady state value or disappeared completely.

Key words: HEK293, patch-clamp, human ether-a-go-go related gene 2, delayed rectifier potassium channel, cisapride

CLC Number:

Yuan Shasha, Huang Haixia, Yang Jinkui. Effects of the gastrointestinal prokinetic agent cisapride on human ether-a-go-go related gene 2 channels expressed on HEK293 cells[J]. Journal of Capital Medical University, 2014, 35(6): 760-764.

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Effects of the gastrointestinal prokinetic agent cisapride on human ether-a-go-go related gene 2 channels expressed on HEK293 cells

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