Characterization of Tachykinin NK sub 2 Receptors in Human Urinary Bladder

No AccessJournal of UrologyInvestigative Urology1 May 1995Characterization of Tachykinin NK sub 2 Receptors in Human Urinary Bladder Xiang-Ping Zeng, Kate H. Moore, and Elizabeth Burcher Xiang-Ping ZengXiang-Ping Zeng More articles by this author , Kate H. MooreKate H. Moore More articles by this author , and Elizabeth BurcherElizabeth Burcher More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(01)67505-0AboutFull TextPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail Functional and radioligand binding studies with selective agonists and antagonists were used to investigate tachykinin receptors in the human bladder. Strips of detrusor muscle were contracted by the tachykinins neurokinin A and neuropeptide gamma, and by the NK2 receptor selective agonists [Lys5, MeLeu9, Nle10]-NKA(4-10) and [Lys5, Tyr(I sub 2)7, MeLeu9, Nle10]-NKA(4-10), with pD2 values 8.2, 8.0, 8.1 and 7.1. [Sar9, Met(O2)11]-SP and senktide were ineffective agonists, indicating an absence of NK1 and NK3 receptors. The contractile responses to [Lys5, MeLeu9, Nle10]-NKA(4-10) were inhibited competitively by the NK2 receptor selective antagonists SR 48968, GR 94800 and MDL 29913, with pA2 values 9.1, 8.6 and 7.0. Specific binding of the new NK2 receptor selective radioligand [sup 125 I]-[Lys5, Tyr(I2)7, MeLeu9, Nle10]-NKA(4-10) was saturable to a high affinity site (KD 2.3 nM.). Specific binding was inhibited by NK2 receptor agonists and antagonists, but not by NK1 and NK3 analogues, showing binding to NK2 receptors only. These data indicate that NK2 receptors may be involved in regulation of detrusor contractility in the human bladder. References 1 : Tachykinin receptors: a radioligand binding perspective.. J. Neurochem.1993; 60: 1987. Google Scholar 2 : Effects of active peptides in the isolated muscle of the human urinary bladder.. Invest. Urol.1981; 18: 302. 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Google Scholar From the School and Physiology and Pharmacology, and The Pelvic Floor Unit, Department of Obstetrics and Gynaecology, St. George Hospital, University of New South Wales, Sydney, Australia.© 1995 by American Urological Association, Inc.FiguresReferencesRelatedDetailsCited byYOKOYAMA O, YUSUP A, MIWA Y, OYAMA N, AOKI Y and AKINO H (2018) EFFECTS OF TOLTERODINE ON AN OVERACTIVE BLADDER DEPEND ON SUPPRESSION OF C-FIBER BLADDER AFFERENT ACTIVITY IN RATSJournal of Urology, VOL. 174, NO. 5, (2032-2036), Online publication date: 1-Nov-2005.BURCHER E, ZENG X, STRIGAS J, SHANG F, MILLARD R and MOORE K (2018) AUTORADIOGRAPHIC LOCALIZATION OF TACHYKININ AND CALCITONIN GENE-RELATED PEPTIDE RECEPTORS IN ADULT URINARY BLADDERJournal of Urology, VOL. 163, NO. 1, (331-337), Online publication date: 1-Jan-2000.Zeng X and Burcher E (2018) Tachykinin NK-2 Receptors in Child Urinary BladderJournal of Urology, VOL. 155, NO. 3, (1104-1107), Online publication date: 1-Mar-1996. Volume 153Issue 5May 1995Page: 1688-1692 Advertisement Copyright & Permissions© 1995 by American Urological Association, Inc.MetricsAuthor Information Xiang-Ping Zeng More articles by this author Kate H. Moore More articles by this author Elizabeth Burcher More articles by this author Expand All Advertisement PDF downloadLoading ...