Stasch J P, Steinke W, Kazda S, Neuser D
Institut of Pharmacology, Bayer AG, Wuppertal, Fed. Rep. of Germany.
Arzneimittelforschung. 1991 May;41(5):478-80.
Endothelin-1 (ET-1), a potent vasoconstrictor with a characteristically long-acting activity in vitro and in vivo, is thought to be generated in endothelial cells from a less active intermediate, big endothelin-1 (big ET-1). In addition to ET-1, big ET-1 is also present in the circulation. The autoradiographic localization of 125I-big ET-1 has been studied after intravenous administration in rat tissues. Highest enrichment of radioactivity was found in the kidney cortex. Compared to blood levels, enrichment of radioactivity is also detected, especially in the vascular wall of the aorta. Comparing the radioactivity pattern of ET-1 and big ET-1, a nearly identical tissue distribution is observed, with the exception of the relative enrichment in the lung, the endocardium and the zona glomerulosa.
内皮素 -1(ET -1)是一种强效血管收缩剂,在体外和体内均具有典型的长效活性,被认为是由活性较低的中间体大内皮素 -1(big ET -1)在内皮细胞中生成的。除了ET -1,big ET -1也存在于循环系统中。在大鼠组织中静脉注射125I - big ET -1后,对其放射自显影定位进行了研究。在肾皮质中发现放射性富集最高。与血液水平相比,在主动脉血管壁等部位也检测到放射性富集。比较ET -1和big ET -1的放射性分布模式,观察到除了在肺、心内膜和肾小球带中的相对富集情况外,两者的组织分布几乎相同。