Gray G A, Webb D J
Department of Pharmacology, University of Edinburgh, Scotland.
Pharmacol Ther. 1996;72(2):109-48. doi: 10.1016/s0163-7258(96)00101-5.
Endothelin (ET)-1, an endothelium-derived peptide, is the most potent vasoconstrictor agent described to date. ET-1 also has positive inotropic and chronotropic effects in the heart and is a co-mitogen in both cardiac and vascular myocytes. The major elements of the system involved in formation of ET-1 and its isopeptides, as well as the receptors mediating their effects, have been cloned and characterised. Antagonists of the ET receptors are now available, and selective inhibitors of the ET-converting enzymes are being developed. Early studies using receptor antagonists support the involvement of ET-1 in the pathophysiology of several cardiovascular diseases. The relative merits of ET-converting enzyme inhibitors and receptor antagonists for the treatment of cardiovascular disease are discussed.
内皮素（ET）-1是一种内皮衍生肽，是迄今为止所描述的最有效的血管收缩剂。ET-1对心脏也有正性肌力和变时作用，并且在心脏和血管肌细胞中都是一种协同促分裂原。参与ET-1及其异肽形成的系统的主要成分，以及介导其作用的受体，已被克隆和鉴定。ET受体拮抗剂现已可用，并且正在开发ET转换酶的选择性抑制剂。使用受体拮抗剂的早期研究支持ET-1参与几种心血管疾病的病理生理学。本文讨论了ET转换酶抑制剂和受体拮抗剂在治疗心血管疾病方面的相对优点。
