Urocontrin, a novel UT receptor ligand with a unique pharmacological profile
Urocontrin, a novel UT receptor ligand with a unique pharmacological profile
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DOI：
10.1016/j.bcp.2011.12.009
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发表时间：
2012-03-01
影响因子：
5.8
通讯作者：
Fournier, Alain
中科院分区：
文献类型：
--
作者：
Chatenet, David;Quang-Trinh Nguyen;Fournier, Alain
近年来，一些研究表明尾加压素II(UII)和尾加压素II相关肽(URP)具有不同的生物学活性。到目前为止，已知的尾加压素11受体(UT)拮抗剂在研究UII或URP的具体病理生理作用方面的作用有限。因此，鉴定能够区分UII和URP相关生物活性的新化合物是非常必要的。在本研究中，我们报道了一种名为尿囊素的新型UT配体的药理性质的初步数据，即[Bip(4)]URP，它能降低hUII诱导的大鼠主动脉环血管收缩的体外效应，但不能降低URP引起的血管收缩。体内研究支持上述药理学特征。虽然尿激肽仍具有一定的激动剂活性，但该化合物可用于合理设计有效的分子，以区分UII或URP介导的特定生物学作用。(C)2011 Elsevier Inc.保留所有权利。
In recent years, several studies have demonstrated that urotensin II (UII) and urotensin II-related peptide (URP) can exhibit differential biological activity. So far, known antagonists of the urotensin 11 receptor (UT) are of limited usefulness for investigating the specific pathophysiological role of UII or URP. Therefore, identification of new compounds able to discriminate UII- and URP-associated biological activities is crucially needed. In the present study, we report preliminary data regarding the pharmacological properties of a novel UT ligand termed urocontrin, i.e. [Bip(4)]URP, that is able to reduce the ex vivo efficacy of hUII- but not URP-induced vasoconstriction in rat aortic rings. In vivo studies support the pharmacological profile described above. Although urocontrin exert some residual agonist activity, this compound should be useful for the rational design of potent molecules that would allow discriminating specific biological action mediated by UII or URP. (C) 2011 Elsevier Inc. All rights reserved.