The effects of N-terminal part modification of arginine vasopressin analogues with 2-aminoindane-2-carboxylic acid: a highly potent V2 agonist.
In this study we present the synthesis and some pharmacological properties of nine new analogues of arginine vasopressin modified in the N-terminal part of the molecule with 2-aminoindane-2-carboxylic acid (Aic). The peptides were tested for their in vitro uterotonic and in vivo pressor and antidiuretic activities. One of the new peptides, [Mpa1,Aic2,Val4,D-Arg8]VP, exhibited an antidiuretic activity similar to that of [Mpa1,D-Arg8]VP, thus being one of the most potent antidiuretic vasopressin analogues reported to date.
Kowalczyk
Wioleta
W
Faculty of Chemistry, University of Gdańsk, Sobieskiego 18, 80-952 Gdańsk, Poland. wiola@chem.univ-gda.pl
Sobolewski
Dariusz
D
Prahl
Adam
A
Derdowska
Izabela
I
Borovicková
Lenka
L
Slaninová
Jirina
J
Lammek
Bernard
B
D000818:Animals; D050034:Antidiuretic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D065092:Antidiuretic Hormone Receptor Antagonists; D001127:Arginine Vasopressin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D066298:In Vitro Techniques; D011487:Protein Conformation; D051381:Rats; D017208:Rats, Wistar; D017483:Receptors, Vasopressin / Q000819:agonists*; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects
C480478:2-aminoindane-2-carboxylic acid; D050034:Antidiuretic Agents; D065092:Antidiuretic Hormone Receptor Antagonists; D002264:Carboxylic Acids; D017483:Receptors, Vasopressin; C521972:vasopressin, Mpa(1)-Aic(2)-Val(4)-Arg(8)-; D001127:Arginine Vasopressin