As part of a program to design potent antidiuretic vasopressin antagonists and to define the minimum effective pharmacophore requirements for vasopressin (VP) antagonist activity, we studied the importance of the C-terminal tripeptide of a previously reported peptide antagonist of arginiie-vasopressin (AVP, 1). The proline residue at position 7 in AVP is proposed to impart a conformational constraint to the peptide backbone that is essential ...
