Cyclic and linear vasopressin V1 and V1/V2 antagonists containing arginine in the 4-position.

作者信息

Sawyer W H, Lammek B, Misicka A, Kruszynski M, Kolodzieczyk A, Manning M

机构信息

Department of Pharmacology, College of Physicians and Surgeons of Columbia University, New York, New York 10032.

出版信息

Experientia. 1991 Jan 15;47(1):83-6. doi: 10.1007/BF02041261.

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.