HYPERPOLARIZING VASODILATORS ACTIVATE ATP-SENSITIVE K+ CHANNELS IN ARTERIAL SMOOTH-MUSCLE
HYPERPOLARIZING VASODILATORS ACTIVATE ATP-SENSITIVE K+ CHANNELS IN ARTERIAL SMOOTH-MUSCLE
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DOI：
10.1126/science.2501869
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发表时间：
1989-07-14
期刊：
影响因子：
56.9
通讯作者：
NELSON, MT
中科院分区：
文献类型：
--
作者：
STANDEN, NB;QUAYLE, JM;NELSON, MT
血管扩张剂在临床上用于治疗高血压和心力衰竭。一些血管扩张剂的作用似乎是通过膜超极化介导的。这种超极化的分子基础已被研究，通过检查动脉平滑肌细胞中的单个K+通道的特性。在单通道水平上证明了这些细胞中存在三磷酸腺苷（ATP）敏感性K+通道。这些通道开放的超极化血管扩张剂cromakalim和抑制ATP敏感的K+通道阻滞剂格列本脲。此外，在动脉环中，药物二氮嗪、色满卡林和吡那地尔的血管舒张作用以及血管活性肠多肽和乙酰胆碱的超极化作用被ATP敏感性K+通道抑制剂阻断，表明所有这些药物可能通过开放ATP敏感性K+通道的共同途径在平滑肌中起作用。
Vasodilators are used clinically for the treatment of hypertension and heart failure. The effects of some vasodilators seem to be mediated by membrane hyperpolarization. The molecular basis of this hyperpolarization has been investigated by examining the properties of single K+ channels in arterial smooth muscle cells. The presence of adenosine triphosphate (ATP)-sensitive K+ channels in these cells was demonstrated at the single channel level. These channels were opened by the hyperpolarizing vasodilator cromakalim and inhibited by the ATP-sensitive K+ channel blocker glibenclamide. Furthermore, in arterial rings the vasorelaxing actions of the drugs diazoxide, cromakalim, and pinacidil and the hyperpolarizing actions of vasoactive intestinal polypeptide and acetylcholine were blocked by inhibitors of the ATP-sensitive K+ channel, suggesting that all these agents may act through a common pathway in smooth muscle by opening ATP-sensitive K+ channels.