Yang Z H, Bühler F R, Diederich D, Lüscher T F
Department of Research, University Hospitals, Basel, Switzerland.
J Cardiovasc Pharmacol. 1989;13 Suppl 5:S129-31; discussion S142. doi: 10.1097/00005344-198900135-00032.
Endothelin-1 (ET-1) is a new cardiovascular hormone produced by endothelial cells. The vascular effects of the peptide and its interaction with cAMP- and cGMP-dependent relaxation were investigated in human arteries and veins. Internal mammary arteries and veins and saphenous veins were obtained intraoperatively and suspended in organ chambers; isometric tension was recorded. The blood vessels were contracted with ET-1 or norepinephrine and relaxations to prostacyclin or sodium nitroprusside were studied. Mammary veins exhibited an enhanced sensitivity to ET-1 (10(-11) to 3 X 10(-7) M) as compared to the artery and saphenous vein (log shift at ED50: 32- and 79-fold, respectively; p less than 0.005). In saphenous veins maximally contracted with ET-1, relaxations to prostacyclin were blunted as compared to the artery (p less than 0.005; n = 5). Similarly, ET-1 inhibited relaxations to sodium nitroprusside in the vein, but not in the artery. In contrast, venous rings contracted with norepinephrine were more sensitive to sodium nitroprusside than the artery. Thus, the human mammary vein, but not the saphenous vein, is more sensitive to the vasoconstrictor effects of ET-1 when compared to the mammary artery. In veins, ET-1 but not norepinephrine inhibits the vascular effects of prostacyclin and sodium nitroprusside, suggesting a specific interaction of the peptide with cAMP- and cGMP-dependent relaxation.
内皮素-1（ET-1）是一种由内皮细胞产生的新型心血管激素。研究了该肽的血管效应及其与环磷酸腺苷（cAMP）和环磷酸鸟苷（cGMP）依赖性舒张的相互作用，实验对象为人体的动脉和静脉。术中获取乳内动脉和静脉以及大隐静脉，并将其悬挂于器官浴槽中；记录等长张力。用ET-1或去甲肾上腺素使血管收缩，然后研究血管对前列环素或硝普钠的舒张反应。与动脉和大隐静脉相比，乳静脉对ET-1（10^(-11)至3×10^(-7) M）表现出更高的敏感性（半数有效剂量（ED50）的对数位移分别为32倍和79倍；p<0.005）。在被ET-1最大程度收缩的大隐静脉中，与动脉相比，对前列环素的舒张反应减弱（p<0.005；n = 5）。同样，ET-1抑制静脉对硝普钠的舒张反应，但不抑制动脉的。相反，用去甲肾上腺素收缩的静脉环对硝普钠的敏感性高于动脉。因此，与乳动脉相比，人乳静脉而非大隐静脉对ET-1的血管收缩作用更敏感。在静脉中，ET-1而非去甲肾上腺素抑制前列环素和硝普钠的血管效应，提示该肽与cAMP和cGMP依赖性舒张存在特异性相互作用。
