Masaki T
Institute of Basic Medical Sciences, University of Tsukuba, Japan.
J Cardiovasc Pharmacol. 1989;13 Suppl 5:S1-4; discussion S18. doi: 10.1097/00005344-198900135-00002.
Endothelin-1 (ET-1) is a potent vasoconstrictive peptide produced by endothelial cells of blood vessels. This peptide has quite a unique structure and pharmacological properties. ET-1 is produced in endothelial cells and may be secreted in a similar way to some paracrine hormones. The pressor response of ET-1 is largely ascribed to its direct vasoconstrictive activity. However, renin release induced by vasoconstriction of the renal artery and elevation of sympathetic tone via central nervous system stimulation by ET-1 are also possible causes of the pressor responses. ET-1 receptors and calcium channels are different. Activation of these receptors may stimulate calcium stores via phosphatidylinositol (PI) turnover, inducing a transient increase of intracellular free calcium as well as initiating a calcium influx via the cell membrane calcium channel. The latter calcium influx induces the sustained increase of intracellular calcium ion and contracture. Recent experimental results suggest the possibility that ET has extracardiovascular activities in addition to its cardiovascular effect, i.e., it may be a neuropeptide or a neurosecretory hormone. ET-1 is also a cell-growth factor.
内皮素 -1（ET -1）是一种由血管内皮细胞产生的强效血管收缩肽。这种肽具有相当独特的结构和药理特性。ET -1在内皮细胞中产生，并可能以与某些旁分泌激素类似的方式分泌。ET -1的升压反应很大程度上归因于其直接的血管收缩活性。然而，肾动脉血管收缩引起的肾素释放以及ET -1通过中枢神经系统刺激引起的交感神经张力升高也是升压反应的可能原因。ET -1受体和钙通道不同。这些受体的激活可能通过磷脂酰肌醇（PI）周转刺激钙储存，导致细胞内游离钙短暂增加，并通过细胞膜钙通道引发钙内流。后者的钙内流诱导细胞内钙离子持续增加和挛缩。最近的实验结果表明，ET除了具有心血管作用外，还可能具有心血管外活性，即它可能是一种神经肽或神经分泌激素。ET -1也是一种细胞生长因子。
