The effects of N-terminal part modification of arginine vasopressin analogues with 2-aminoindane-2-carboxylic acid:: A highly potent V2 agonist

被引:16
|
作者
Kowalczyk, Wioleta
Sobolewski, Dariusz
Prahl, Adam
Derdowska, Izabela
Borovickova, Lenka
Slaninova, Jirina
Lammek, Bernard
机构
[1] Univ Gdansk, Fac Chem, PL-80952 Gdansk, Poland
[2] Acad Sci Czech Republ, Inst Organ Chem & Biochem, CR-16610 Prague, Czech Republic
关键词
D O I
10.1021/jm070174s
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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, [Mpa(1),Aic(2),Val(4),D-Arg(8)]VP, exhibited an antidiuretic activity similar to that of [Mpa(1),D-Arg(8)]VP, thus being one of the most potent antidiuretic vasopressin analogues reported to date.
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收藏
页码:2926 / 2929
页数:4
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