Cyclic and linear vasopressin V1 and V1/V2 antagonists containing arginine in the 4-position.
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.
Sawyer
W H
WH
Department of Pharmacology, College of Physicians and Surgeons of Columbia University, New York, New York 10032.
Lammek
B
B
Misicka
A
A
Kruszynski
M
M
Kolodzieczyk
A
A
Manning
M
M
D000595:Amino Acid Sequence; D001120:Arginine; D001127:Arginine Vasopressin / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D007202:Indicators and Reagents; D008969:Molecular Sequence Data; D009904:Optical Rotation; D011487:Protein Conformation; D013329:Structure-Activity Relationship; D014667:Vasopressins / Q000037:antagonists & inhibitors* / Q000138:chemical synthesis*
D007202:Indicators and Reagents; D014667:Vasopressins; D001127:Arginine Vasopressin; D001120:Arginine