A conformationally constrained vasopressin analog with antidiuretic antagonistic activity.
Application of information derived from a three-dimensional model of vasopressin bound to its antidiuretic receptor resulted in the design and synthesis of a bicyclic vasopressin analog, [5,8-cyclo(1-beta-mercaptopropionic acid,2-phenylalanine,5-aspartic acid,8-lysine)]vasopressin. The analog acts as an antagonist of the antidiuretic activity of vasopressin.
D000818:Animals; D001127:Arginine Vasopressin / Q000031:analogs & derivatives*; D008236:Lypressin / Q000031:analogs & derivatives*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D001127:Arginine Vasopressin; D008236:Lypressin