首页> 外文期刊>Journal of Medicinal Chemistry >The effects of N-terminal part modification of arginine vasopressin analogues with 2-aminoindane-2-carboxylic acid: A highly potent V-2 agonist
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The effects of N-terminal part modification of arginine vasopressin analogues with 2-aminoindane-2-carboxylic acid: A highly potent V-2 agonist

机译:2-氨基茚满-2-羧酸对精氨酸加压素类似物N末端部分的修饰作用:高效V-2激动剂

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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.
机译:在这项研究中,我们介绍了精氨酸加压素的九种新类似物的合成及其一些药理学性质,该类似物在分子的N端部分被2-氨基茚满-2-羧酸(Aic)修饰。测试了这些肽的体外子宫缩蛋白和体内加压和抗利尿活性。一种新的肽[Mpa(1),Aic(2),Val(4),D-Arg(8)] VP表现出类似于[Mpa(1),D-Arg(8)的抗利尿活性)] VP,因此是迄今为止报道的最有效的抗利尿血管加压素类似物之一。

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