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Cyclic and linear vasopressin V1 and V1/V2 antagonists containing arginine in the 4-position
Authors:W H Sawyer  B Lammek  A Misicka  M Kruszynski  A Kolodzieczyk  M Manning
Institution:(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.
Keywords:Vasopressin antagonists  V1-antagonists  V2-antagonists  neurohypophysial hormones  arginine
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