2. Academic Validation
  3. Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors

Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors

  • Eur J Pharmacol. 2004 Sep 13;498(1-3):83-6. doi: 10.1016/j.ejphar.2004.07.089.
Valeria Camarda 1,  Wei Song,  Erika Marzola,  Martina Spagnol,  Remo Guerrini,  Severo Salvadori,  Domenico Regoli,  Jonathan P Thompson,  David J Rowbotham,  David J Behm,  Stephen A Douglas,  Girolamo Calo',  David G Lambert
Affiliations

Affiliation

  • 1 Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, via Fossato di Mortara, 19, 44100 Ferrara, Italy.
PMID: 15363979 DOI: 10.1016/j.ejphar.2004.07.089
Abstract

Urotensin-II is the natural ligand of the UT receptor. This novel system is involved in the regulation of cardiovascular functions. Recently, a urotensin-II analog ([Pen5,DTrp7,Orn8]urotensin-II(4-11)) named urantide, has been proposed as a selective and potent UT receptor antagonist. In order to pharmacologically characterize this new compound, urantide was tested on the native UT receptors of the rat aorta and on the human recombinant receptors expressed in CHO cells (CHO(hUT)). Indeed, urantide behaves as a competitive, potent (pA2 8.24), and pure antagonist in the rat aorta bioassay, while as an agonist (pEC50 8.11) in a calcium mobilization assay performed in CHO(hUT) cells. Urantide should be considered a low efficacy partial agonist.

Figures
Products