Kusserow Heike, Unger Thomas
Center for Cardiovascular Research/Institute of Pharmacology and Toxicology, Campus Charité Mitte, Charité- Universitätsmedizin Berlin, Hessische Strasse 3-4, D-10115 Berlin, Germany.
Basic Clin Pharmacol Toxicol. 2004 Jan;94(1):5-12.
Vasoactive peptides with vasoconstrictor properties play an important role in many physiological and pathological conditions. The peptides act via specific receptors, most of them belonging to the group of seven transmembrane G-protein coupled receptors. These receptors have become important targets for drugs developed to inhibit vasoconstrictor actions. Alternatively, compounds which inhibit enzymes generating vasoactive peptides have also been demonstrated to represent valuable therapeutic tools. This review will first describe the properties and distribution of two very potent vasoconstrictors, angiotensin II and endothelin. It will further focus on their receptors and on new drugs, which act as antagonists for these receptors. In addition, the properties of indirectly acting drugs like angiotensin-converting enzyme inhibitors and--in analogy--endothelin-converting enzyme inhibitors will be presented.
具有血管收缩特性的血管活性肽在许多生理和病理状况中发挥着重要作用。这些肽通过特定受体起作用，其中大多数属于七跨膜G蛋白偶联受体家族。这些受体已成为开发用于抑制血管收缩作用的药物的重要靶点。另外，抑制产生血管活性肽的酶的化合物也已被证明是有价值的治疗工具。本综述将首先描述两种非常强效的血管收缩剂——血管紧张素II和内皮素的特性及分布。它将进一步聚焦于它们的受体以及作为这些受体拮抗剂的新药。此外，还将介绍间接作用药物如血管紧张素转换酶抑制剂以及类似的内皮素转换酶抑制剂的特性。
