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Urocontrin, a novel UT receptor ligand with a unique pharmacological profile

Chatenet, David ORCID logoORCID: https://orcid.org/0000-0002-7270-4328; Nguyen, Quang-Trinh; Letourneau, Myriam; Dupuis, Jocelyn et Fournier, Alain (2012). Urocontrin, a novel UT receptor ligand with a unique pharmacological profile Biochemical Pharmacology , vol. 83 , nº 5. pp. 608-615. DOI: 10.1016/j.bcp.2011.12.009.

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Résumé


In recent years, several studies have demonstrated that urotensin II (UII) and urotensin II-related peptide (URP) can exhibit differential biol. activity. So far, known antagonists of the urotensin II receptor (UT) are of limited usefulness for investigating the specific pathophysiol. role of UII or URP. Therefore, identification of new compds. able to discriminate UII- and URP-assocd. biol. activities is crucially needed. In the present study, we report preliminary data regarding the pharmacol. properties of a novel UT ligand termed urocontrin, i.e. [Bip4]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 pharmacol. profile described above. Although urocontrin exert some residual agonist activity, this compd. should be useful for the rational design of potent mols. that would allow discriminating specific biol. action mediated by UII or URP.

Type de document: Article
Mots-clés libres: -
Centre: Centre INRS-Institut Armand Frappier
Date de dépôt: 06 mars 2024 15:31
Dernière modification: 06 mars 2024 15:31
URI: https://espace.inrs.ca/id/eprint/13999

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