title: Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors.
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.
authors.affiliation: Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, via Fossato di Mortara, 19, 44100 Ferrara, Italy.
authors.forename: Valeria
authors.initials: V
authors.lastname: Camarda
authors.forename: Wei
authors.initials: W
authors.lastname: Song
authors.forename: Erika
authors.initials: E
authors.lastname: Marzola
authors.forename: Martina
authors.initials: M
authors.lastname: Spagnol
authors.forename: Remo
authors.initials: R
authors.lastname: Guerrini
authors.forename: Severo
authors.initials: S
authors.lastname: Salvadori
authors.forename: Domenico
authors.initials: D
authors.lastname: Regoli
authors.forename: Jonathan P
authors.initials: JP
authors.lastname: Thompson
authors.forename: David J
authors.initials: DJ
authors.lastname: Rowbotham
authors.forename: David J
authors.initials: DJ
authors.lastname: Behm
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Douglas
authors.forename: Girolamo
authors.initials: G
authors.lastname: Calo'
authors.forename: David G
authors.initials: DG
authors.lastname: Lambert
mesh_terms: D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects / Q000502:physiology; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism*; D006224:Cricetinae; D003412:Cricetulus; D004274:DNA, Recombinant / Q000235:genetics; D004305:Dose-Response Relationship, Drug; D015870:Gene Expression; D066298:In Vitro Techniques; D008297:Male; D010446:Peptide Fragments / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D043562:Receptors, G-Protein-Coupled / Q000235:genetics / Q000502:physiology*; D014579:Urotensins / Q000494:pharmacology*; D014661:Vasoconstriction / Q000187:drug effects
chemical_list: D004274:DNA, Recombinant; D010446:Peptide Fragments; D043562:Receptors, G-Protein-Coupled; C121697:UTS2R protein, human; D014579:Urotensins; C492079:urotensin II (4-11), Pen(5)-Trp(7)-Orn(8)-; C029677:urotensin II; D002118:Calcium