Miyauchi T, Masaki T
Department of Internal Medicine, University of Tsukuba, Ibaraki, Japan.
Annu Rev Physiol. 1999;61:391-415. doi: 10.1146/annurev.physiol.61.1.391.
In this article, we review the basic pharmacological and biochemical features of endothelin and the pathophysiological roles of endothelin in cardiovascular diseases. Development of receptor antagonists has accelerated the pace of investigations into the pathophysiological roles of endogenous endothelin-1 in various diseases, e.g. chronic heart failure, renal diseases, hypertension, cerebral vasospasm, and pulmonary hypertension. In chronic heart failure, the expression of endothelin-1 and its receptors in cardiomyocytes is increased, and treatment with an endothelin receptor antagonist improves survival and cardiac function. Endothelin receptor antagonists also improve other cardiovascular diseases. These results suggest that the interference with endothelin pathway either by receptor blockade or by inhibition of endothelin converting enzyme may provide novel therapeutic drugs strategies for multiple disease states.
在本文中，我们综述了内皮素的基本药理和生化特性，以及内皮素在心血管疾病中的病理生理作用。受体拮抗剂的开发加速了对内源性内皮素-1在各种疾病（如慢性心力衰竭、肾脏疾病、高血压、脑血管痉挛和肺动脉高压）中病理生理作用的研究步伐。在慢性心力衰竭中，心肌细胞中内皮素-1及其受体的表达增加，使用内皮素受体拮抗剂进行治疗可提高生存率并改善心脏功能。内皮素受体拮抗剂还可改善其他心血管疾病。这些结果表明，通过受体阻断或抑制内皮素转换酶来干扰内皮素信号通路可能为多种疾病状态提供新的治疗药物策略。
