Endothelin and endothelin antagonists: potential role in cardiovascular and renal disease.

作者: G. Noll , R.R. Wenzel , T.F. L�scher

DOI: 10.1007/BF00227908

关键词: EndotheliumEndothelin receptor antagonistInternal medicineVascular smooth muscleVasodilationEndocrinologyEndothelin 1EndothelinsEndothelin receptorChemistryCyclic guanosine monophosphate

摘要: Endothelin-1 is a recently discovered peptide mainly released from endothelial cells. Hypoxia and ischemia as well numerous factors such angiotensin 11, thrombin transforming growth factor β1 stimulate the fomation of peptide. On other hand synthesis endothelin inhibited by nitric oxide atrial natriuretic via formation cyclic guanosine monophosphate. Released cells endothelin-1 mediates transient vasodilation followed profound longlasting vasoconstriction. Endothelin also mitogen for smooth muscle proliferation. Endothelins exert their biological effects activation specific receptors. Two different receptors have been cloned mammalian tissues (ETA ETB receptors). vascular both mediate contractions. Endothelial only express linked to and/or prostacyclin formation. Increased plasma concentrations described in variety diseases pulmonary hypertension, arteriosclerosis, renal failure, acute coronary syndromes, heart migraine diseases.

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