A Minor Modification of Residue 1 in Potent Vasopressin Antagonists Dramatically Reduces Agonist Activity

Article abstract of DOI:10.1021/jm00124a025

<1-(β,β-Pentamethylene-β-mercaptopropionic acid),2-(O-ethyl)-D-tyrosine,4-valine,9-desglycine>arginine-vasopressin (SK&F 101926, 1), a potent in vivo and in vitro vasopressin V₂ receptor antagonist, was recently tested in human volunteers and s