(1) Department of Pharmacology, College of Physicians and Surgeons of Columbia University, 10032 New York, New York, USA;(2) Department of Biochemistry, Medical College of Ohio, 43699 Toledo, Ohio, USA
Abstract:
Summary Substitution of arginine for glutamine in the 4-position of a vasopressin V1 antagonist has been reported to turn it into an agonist. We resynthesized this 4-arginine analog and synthesized additional cyclic and linear vasopressin antagonists containing a 4-arginine. The presence of a 4-arginine in the resynthesized and new analogs had relatively minor effects on their antivasopressin V1 and V2 antagonistic potencies.