Synthesis and some pharmacological properties of new V1/V2 antagonists of arginine-vasopressin with structural changes at their N-terminals.

B Lammek, E Konieczna, T Wierzba, Y X Wang, H Gavras
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Abstract

In an effort to develop more effective and selective V2-antagonists of arginine-vasopressin (AVP) we designed and synthesized four new analogs of this hormone. The peptides were designed in order to explore how the combination of modification of thioacids occupying position 1 and substitutions of positions 2 and 4 by D-Phe and Ile respectively, will influence their antagonistic properties. Three of the reported analogs are moderately potent V1/V2 antagonists.

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新型精氨酸-抗利尿激素V1/V2拮抗剂的合成及其n端结构变化的药理学性质
为了开发更有效和选择性的精氨酸-抗利尿激素(AVP)的v2拮抗剂,我们设计并合成了四种新的精氨酸-抗利尿激素类似物。设计这些肽的目的是为了探索占据1号位置的硫酸修饰和分别被D-Phe和Ile取代的2号和4号位置的组合如何影响它们的拮抗性能。报道的三种类似物是中等效力的V1/V2拮抗剂。
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