中国病理生理杂志2012，Vol.28Issue(1)：6-10,5.DOI:10.3969/j.issn.1000-4718.2012.01.002
Zacopride增强心肌内向整流钾电流(IK1)效应的受体和信号转导通路
Receptor and signaling mechanisms involved in zacopride-induced potentiation of IK1
摘要
Abstract
ATM:To investigate the receptor and signaling mechanisms involved in the potentiation of inward rectifier K+ current (IK1) induced by zacopride, a potent 5 - HT3 receptor antagonist and 5 - HT4 receptor agonist. METHODS: The whole - cell patch clamp technique was used to record IK1. 5 - HT4 - receptor antagonist RS23597 - 190, 5 - HT3 - receptor agonist m - chlorophenylbiguanide ( m - CPBG ), PKA inhibitor KT5720, PKC inhibitor GF109203X and PKG inhibitor KT5823 were applied respectively to determine the regulatory mechanism of IK1. RESULTS; In the presence of RS23597 - 190 at concentration of 10μmol/L which inhibited IK1 , zacopride at concentration of 1 (xmol/L still increased IK1 with the mean increment of 32. 5% in inward current (at - 100 mV, P <0. 05 ). The IK1 increment induced by zacopride was not inhibited by m - CPBG at concentration of 10 (xmol/L ( P >0. 05 ). Furthermore, PKA inhibitor KT5720 at concentration of 5μmol/L reversed the effect of zacopride ( P < 0. 05 ), while PKC inhibitor GF109203X and PKG inhibitor KT5823 both at concentration of 5μmol/L didn't influence the effect ( P > 0. 05 ). CONCLUSION: Zacopride potentiates IK1 via a PKA - mediated signaling pathway, which is independent on 5 - HT4 and 5 - HT3 receptors.关键词
内向整流钾通道/Zacopride/受体,5-HTKey words
Inward rectifier K+ current/Zacopride/Receptors,5-HT分类
医药卫生引用本文复制引用
刘清华,许言午,吴博威..Zacopride增强心肌内向整流钾电流(IK1)效应的受体和信号转导通路[J].中国病理生理杂志,2012,28(1):6-10,5.基金项目
国家自然科学基金资助项目(No.30840038) （No.30840038）
山西省自然科学基金青年项目(No.2009021043-2) （No.2009021043-2）
