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Endothelin in the Urinary Bladder. II. Characterization of Endothelin Receptor Subtypes

1992; Lippincott Williams & Wilkins; Volume: 148; Issue: 4 Linguagem: Inglês

10.1016/s0022-5347(17)36896-9

1527-3792

Abdulmaged M. Traish, Elizabeth Morán, Robert J. Krane, Iñigo Sáenz de Tejada,

Neuropeptides and Animal Physiology

No AccessJournal of Urology1 Oct 1992Endothelin in the Urinary Bladder. II. Characterization of Endothelin Receptor Subtypes Abdulmaged Traish, Elizabeth Moran, Robert J. Krane, and Iñigo Saenz de Tejada Abdulmaged TraishAbdulmaged Traish More articles by this author , Elizabeth MoranElizabeth Moran More articles by this author , Robert J. KraneRobert J. Krane More articles by this author , and Iñigo Saenz de TejadaIñigo Saenz de Tejada More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(17)36896-9AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail Endothelins (ET-1, ET-2, ET-3) are a family of regulatory peptides with diverse biological functions, including modulation of smooth muscle tone. To evaluate the possible role of endothelins in the control of the detrusor smooth muscle of urinary bladder, we have investigated the responses of isolated strips of bladder dome and base to endothelins, in organ chambers, and characterized the receptors for these isopeptides in bladder membranes. ET-1, ET-2 and to a lesser extent ET-3 caused sustained concentration-dependent contraction of bladder dome and base. The contraction to endothelins, unlike the short-lived contraction produced by cholinergic agents, was long lasting and difficult to wash out. Equilibrium binding studies demonstrated that endothelin isoforms bound to bladder membrane receptors specifically, with high affinity (KD of 0.4–0.6nM) and limited capacity (60-420 fmol/mg protein). Competition analysis showed two populations of receptors: one with high affinity for ET-1 and ET-2 and low affinity for ET-3 and another with high affinity for ET-1, ET-2 and ET-3. Chemical affinity labeling of endothelins to bladder membranes demonstrated that ET-1 and ET-2 were cross-linked to three proteins (75, 52 and 34kDa, respectively), whereas ET-3 was cross-linked mainly to a 34kDa protein. The data obtained from equilibrium binding studies, competition analysis and cross-linking experiments suggest that at least two endothelin receptor subtypes exist in bladder tissue. These observations further suggest that bladder smooth muscle tone may be modulated by endothelin or an endothelin-like substance via interaction with specific receptor sites. © 1992 by The American Urological Association Education and Research, Inc.FiguresReferencesRelatedDetailsCited ByKobayashi S, Tang R, Wang B, Opgenorth T, Stein E, Shapiro E and Lepor H (2018) Localization of Endothelin Receptors in the Human ProstateJournal of Urology, VOL. 151, NO. 3, (763-766), Online publication date: 1-Mar-1994.De Tejada I, Mueller J, De Las Morenas A, Machado M, Moreland R, Krane R, Wolfe H and Traish A (2018) Endothelin in the Urinary Bladder. I. Synthesis of Endothelin-1 by Epithelia, Smooth Muscle and Fibroblasts Suggests Autocrine and Paracrine Cellular RegulationJournal of Urology, VOL. 148, NO. 4, (1290-1298), Online publication date: 1-Oct-1992. Volume 148Issue 4October 1992Page: 1299-1306 Advertisement Copyright & Permissions© 1992 by The American Urological Association Education and Research, Inc.KeywordsnervesbladderendothelinsMetricsAuthor Information Abdulmaged Traish More articles by this author Elizabeth Moran More articles by this author Robert J. Krane More articles by this author Iñigo Saenz de Tejada More articles by this author Expand All Advertisement Loading ...