Vasoactive Peptides, their Receptors and Drug Development

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.