κ-阿片受体激动通过激活K_(ATP)通道对大鼠腹主动脉产生舒张作用(英文)

κ-Opioid receptor stimulation contributes to aortic artery dilation through activation of K_(ATP) channel in the rats

为观察U5 0 ,488H(选择性κ 阿片受体激动剂 )对大鼠腹主动脉的舒张作用 ,并探讨其机制 ,实验采用离体血管灌流实验 ,测定血管张力的改变。结果显示 :(1)U5 0 ,488H对大鼠腹主动脉具有明显的舒张作用 ;(2 )U5 0 ,488H对大鼠腹主动脉的舒张效应部分依赖于内皮细胞的存在 ;(3 )优降糖和格列甲嗪可明显抑制U5 0 ,488H对大鼠腹主动脉的舒张作用 ;(4)U5 0 ,488H的舒张血管效应与M受体、β受体、前列腺素及NO无关。结果表明 ,U5 0 ,488H是一种有效的扩血管物质 ,其舒张血管的效应具有内皮依赖性 。

To investigate the relaxation effect and underlying mechanism of U50,488H (a selective κ opioid receptor agonist) on aorta in the rat, isolated aortic ring was perfused and the tension of the vessel was measured. It was shown: (1) κ opioid receptor stimulation with U50,488H relaxed rat aorta dose dependently; (2) the relaxation effect of U50,488H on aorta was partially endothelium dependent; (3) the relaxation effect of U50,488H was significantly attenuated in the presence of glybenclamide and glipizide, two ATP sensitive K + channel (K ATP ) blockers; and (4) the relaxation effect of U50,488H on vessel bore no relationship to muscarinic receptor, β adrenoceptor, prostaglandin and nitric oxide (NO). These results indicate that κ opioid receptor stimulation with U50,488H relaxes the aortic artery at least partially via K ATP channel in the rat.