Shah Rahman
Section of Cardiovascular Medicine, Department of Medicine, Brigham and Women's Hospital, Harvard Medical School, 75 Francis Street, Boston, MA 02115, USA.
Eur J Intern Med. 2007 Jul;18(4):272-82. doi: 10.1016/j.ejim.2007.04.002.
Endothelins are powerful vasoconstrictor peptides that also play numerous other roles. The endothelin (ET) family consists of three peptides produced by a variety of tissues. Endothelin-1 (ET-1) is the principal isoform produced by the endothelium in the human cardiovascular system, and it exerts its actions through binding to specific receptors, the so-called type A (ET(A)) and type B (ET(B)) receptors. ET-1 is primarily a locally acting paracrine substance that appears to contribute to the maintenance of basal vascular tone. It is also activated in several diseases, including congestive heart failure, arterial hypertension, atherosclerosis, endothelial dysfunction, coronary artery diseases, renal failure, cerebrovascular disease, pulmonary arterial hypertension, and sepsis. Thus, ET-1 antagonists are promising new agents. They have been shown to be effective in the management of primary pulmonary hypertension, but disappointing in heart failure. Clinical trials are needed to determine whether manipulation of the ET system will be beneficial in other diseases.
内皮素是强大的血管收缩肽，还发挥着许多其他作用。内皮素（ET）家族由多种组织产生的三种肽组成。内皮素-1（ET-1）是人类心血管系统中内皮细胞产生的主要同种型，它通过与特定受体（即所谓的A型（ET(A)）和B型（ET(B)）受体）结合来发挥作用。ET-1主要是一种局部起作用的旁分泌物质，似乎有助于维持基础血管张力。它还在多种疾病中被激活，包括充血性心力衰竭、动脉高血压、动脉粥样硬化、内皮功能障碍、冠状动脉疾病、肾衰竭、脑血管疾病、肺动脉高压和脓毒症。因此，ET-1拮抗剂是有前景的新型药物。它们已被证明在原发性肺动脉高压的治疗中有效，但在心力衰竭治疗中效果不佳。需要进行临床试验来确定对ET系统的调控在其他疾病中是否有益。
