血管平滑肌ATP敏感性钾通道研究进展

ATP敏感性钾通道 (KATP)广泛存在于各类细胞和组织中 ,是药物作用的重要靶点。KATP是由内向整流钾通道Kir和磺酰脲类受体SUR亚基组成。与血管舒缩特性密切相关的是SUR2B/Kir6 1,电导值小 ,对ATP的抑制作用不敏感 ,需要有NDP才能被开放 ,故这类血管平滑肌KATP又被称为NDP依赖性钾通道。内源性和外源性的很多因子引起的血管舒缩反应与血管平滑肌上的KATP有关 ,此信号途径与PKA、PKC等磷酸化激酶有密切联系。不同血管对钾通道开放剂(potassiumchannelopeners,KCO)的反应有差异 ,KCO对血管的选择性作用机制仍不明确。本文就血管平滑肌KATP的分子结构、电生理、药理学特征、信号转导途径和KCO对血管的选择性作用进行综述

Progress in vascular smooth muscle ATP-sensitive potassium channel

ATP sensitive potassium channel(K ATP has been indentified in a variety of tissues and recognized as an important drug target.K ATP channels is composed with a 4∶4 stoichiometry of an inwardly rectifying K + channel(Kir) subunit plus a sulfonylurea receptor(SUR).The characteristics for the SUB2B/Kir 6 1 in vascular are small condutance,ATP insensitivity and activation by added NDP.Therefore,it is refered as NDP dependent K + channel(K NDP ).A lot of endogenous and exogenous vasodilators seem to act through a common pathway by opening K ATP in vascular,which is involved in protein kinase A and C signal transduction pathway.Vascular shows different sensitivity to potassium channel openers(KCO),and the mechanism remains to be determined.In this review,a summary of K ATP in vascular is presented with molecular structure,KCO selectivity to tissue,signal pathway,electrophysiological and pharmacological properties.