胰岛素对Na^+ -H^+交换阻滞剂与钙通道阻滞剂拮抗内皮素-1作用的影响

Influence of insulin on Na^+-H^+ exchange blockers and calcium channel blockers against ET-1 contractive effects

高胰岛素血症(hyperinsulinemia,HIS)在原发性高血压病(essential hyPertension,EH)的发病中起着重要的作用。本实验在病理性高胰岛素及无胰岛素环境中,采用Na^+—H^+交换阻滞剂呋喃苯氨酸(FUR)、布美他尼(BUM)和阿米洛利(AMI)及钙通道阻滞剂维拉帕米(VER)和盐酸川芎嗪(LIG),在离体血管上对内皮素1—(ET—1)缩血管效应的拮抗作用进行了初步研究。实验结果表明:(1)Na^+—H^+交换阻滞剂与钙通道阻滞剂能显著拮抗ET—1的缩血管的效应;(2)舒血管效应呈明显剂量依赖性;(3)Na^+—H^+交换阻滞剂的效能小于钙通道阻滞剂;(4)有无胰岛素对二类药物的舒血管作用无明显影响;(5)在无胰岛素环境中,舒血管作用的大小顺序为VER>LIG>AMI>BUM>FUR;而在高胰岛素环境中,舒血管作用大小顺序为VER>LIG>FUR>AMI>BUM。

Na+ -H + exchange blockers furosemide (FUR), bumetanide (BUM), amiloride (AMI) and calcium channel blockers verapamil (VER), ligustrazine (LIG) against the endothelin-1 (ET - 1) contractile effects on isolated aortic ring of rats with or without insulin was investigated. The results showed that: 1) Na+-H+ exchange blockes and calcium channel blockers inhibited the contractive effects of ET - 1 markedly; 2) Vasodilative effects were in a dose- dependent manner; 3) The potency of Na+ - H+ exchange blockers on vasodilation were smaller than calcium channel blockers; 4) The potency of Na+ -H+ exchange blockers and calcium channel blocker had no difference with or without insulin except FUR; 5) Pharmacodynamic analysis showed that the sequence of vasodilation wereVER>LIG>AMI>BUM>FUR without insulin and VER >LIG>FUR > AMI >BUMwith high insulin level.