Vasopressin Agonists and Antagonists

In this article, the discrete modifications of the structure of the vasopressin molecule which led to the development of specific V1 vascular, V2 renal, and mixed V1/V2 analogs are reviewed. Particularly, the third generation of vasopressin antagonists produced by deletions and substitutions of the carboxy terminal, and the fourth generation of vasopressin antagonists obtained by deletions, substitutions, and the linearization of the molecule are presented. The potential advantages of these different compounds are illustrated by our work on V1 vascular vasopressin receptors of human platelets.