Center for Perinatal Biology, Division of Pharmacology, Department of Basic Sciences, Loma Linda University, School of Medicine, Loma Linda, CA 92350, USA.
Curr Vasc Pharmacol. 2013 Sep;11(5):594-605. doi: 10.2174/1570161111311050004.
Endothelins are 21-amino acid peptides involved in vascular homeostasis. Three types of peptide have been identified, with endothelin-1 (ET-1) being the most potent vasoconstrictor currently known. Two endothelin receptor subtypes are found in various tissues, including the brain, heart, blood vessel, lung, and placenta. The ETA-receptor is associated with vasoconstriction in vascular smooth muscle. Conversely, the ETB-receptor can elicit a vasoconstrictor effect in vascular smooth muscle and a vasodilator effect via its action in endothelial cells. Both receptors play a key role in maintaining circulatory homeostasis and vascular function. Changes in ET-1 expression are found in various disease states, and overexpression of ET-1 is observed in hypertension and preeclampsia in pregnancy. Placental localization of ET-1 implies a key role in regulating the uteroplacental circulation. Additionally, ET-1 is important in the fetal circulation and is involved in the pulmonary circulation and closure of the ductus arteriosus after birth, as well as fetal growth constriction in utero. ET receptor antagonists and nitric oxide donors may provide therapeutic potential in treating conditions associated with overexpression of ET and hypertension.
内皮素是参与血管内稳态的 21 个氨基酸肽。已经鉴定出三种类型的肽，其中内皮素-1（ET-1）是目前已知的最有效的血管收缩剂。两种内皮素受体亚型存在于各种组织中，包括大脑、心脏、血管、肺和胎盘。ETA 受体与血管平滑肌的血管收缩有关。相反，ETB 受体可以通过其在内皮细胞中的作用引起血管平滑肌的血管收缩作用和血管舒张作用。这两种受体在维持循环内稳态和血管功能方面发挥着关键作用。在各种疾病状态下都发现了 ET-1 表达的变化，并且在高血压和妊娠子痫前期中观察到 ET-1 的过度表达。胎盘 ET-1 的定位表明其在调节子宫胎盘循环中具有关键作用。此外，ET-1 在胎儿循环中很重要，参与出生后肺循环和动脉导管关闭，以及胎儿在子宫内生长受限。ET 受体拮抗剂和一氧化氮供体可能在治疗与 ET 过度表达和高血压相关的疾病方面具有治疗潜力。
