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• W2086652365 abstract "No AccessJournal of UrologyINVESTIGATIVE UROLOGY1 Dec 2002Identification of β-Adrenoceptor Subtypes in Lower Urinary Tract of the Female Pig TOMONORI YAMANISHI, CHRISTOPHER R. CHAPPLE, KOSAKU YASUDA, KEN-ICHIRO YOSHIDA, and RUSSELL CHESS-WILLIAMS TOMONORI YAMANISHITOMONORI YAMANISHI More articles by this author , CHRISTOPHER R. CHAPPLECHRISTOPHER R. CHAPPLE More articles by this author , KOSAKU YASUDAKOSAKU YASUDA More articles by this author , KEN-ICHIRO YOSHIDAKEN-ICHIRO YOSHIDA More articles by this author , and RUSSELL CHESS-WILLIAMSRUSSELL CHESS-WILLIAMS More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(05)64248-6AboutFull TextPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail Abstract Purpose: We investigated the presence and functional role of β-adrenoceptor subtypes in the bladder base and proximal urethra of the female pig. Materials and Methods: Saturation experiments were done with 7 concentrations (0.25 to 16 nM.) of [3H]-dihydroalprenolol (NEN Life Science Products, Boston, Massachusetts). Competition experiments with [3H]-dihydroalprenolol were performed with unlabeled antagonists (β1 selective CGP20712A, β2 selective ICI118551 and β3 selective SR59230A). In functional studies concentration-relaxation curves to the β3-agonist BRL37344 were obtained and antagonist affinities for SR59230A were determined. Results: CGP20712A displaced [3H]-dihydroalprenolol with low affinity, suggesting that β1-adrenoceptors were not present. Displacement with ICI118551 in the bladder base and urethra best fitted a 2-site model with 20% and 28% high affinity sites (β2), respectively. Displacement experiments with SR59230A in the bladder base demonstrated that 59% of binding sites had high affinity (β3). In the urethra displacement with SR59230A best fitted a 1-site model but with a pKi of 7.2 that was intermediate between that expected for β2 and β3-adrenoceptors. In functional studies BRL37344 induced relaxation with pEC50 values of 5.5 and 8, and a maximum relaxation response relative to 30 μM. isoprenaline of 79% and 90% in the bladder base and urethra, respectively. The affinity value of SR59230A for the response to BRL37344 was 7.87 and 7.71 in the bladder base and urethra, respectively, which were intermediate between those of β2 and β3-adrenoceptors. Conclusions: Apparently β3-adrenoceptors are the predominant β-adrenoceptor subtype present in the lower urinary tract of the pig. References 1 : Quantitative analysis of alpha and beta adrenergic receptor densities in the lower urinary tract of the dog and the rabbit. Invest Urol1979; 17: 75. Medline, Google Scholar 2 : Expression and possible functional role of the beta3-adrenoceptor in human and rat detrusor muscle. 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Link, Google Scholar From the Department of Biomedical Science, University of Sheffield and Department of Urology, Royal Hallamshire Hospital, Sheffield, United Kingdom, and Department of Urology, Dokkyo University, Japan© 2002 by American Urological Association, Inc.FiguresReferencesRelatedDetailsCited by Mitidieri E, Pecoraro A, Esposito E, Brancaleone V, Turnaturi C, Napolitano L, Mirone V, Fusco F, Cirino G, Sorrentino R, Russo G, Russo A and d’Emmanuele di Villa Bianca R (2022) β3 Relaxant Effect in Human Bladder Involves Cystathionine γ-Lyase-Derived Urothelial Hydrogen SulfideAntioxidants, 10.3390/antiox11081480, VOL. 11, NO. 8, (1480) Wuest M, Eichhorn B, Grimm M, Wirth M, Ravens U and Kaumann A (2008) Catecholamines Relax Detrusor through β 2 -Adrenoceptors in Mouse and β 3 -Adrenoceptors in Man Journal of Pharmacology and Experimental Therapeutics, 10.1124/jpet.108.142562, VOL. 328, NO. 1, (213-222), Online publication date: 1-Jan-2009. Vrydag W and Michel M (2007) Tools to study β3-adrenoceptorsNaunyn-Schmiedeberg's Archives of Pharmacology, 10.1007/s00210-006-0127-5, VOL. 374, NO. 5-6, (385-398), Online publication date: 6-Feb-2007. Seifert R (2007) SR59230A xPharm: The Comprehensive Pharmacology Reference, 10.1016/B978-008055232-3.62673-X, (1-3), . Niclauß N, Michel-Reher M, Alewijnse A and Michel M (2006) Comparison of three radioligands for the labelling of human β-adrenoceptor subtypesNaunyn-Schmiedeberg's Archives of Pharmacology, 10.1007/s00210-006-0104-z, VOL. 374, NO. 2, (99-105), Online publication date: 27-Oct-2006. CHAPPLE C and GORMLEY E (2006) Developments in pharmacological therapy for the overactive bladderBJU International, 10.1111/j.1464-410X.2006.06381.x, VOL. 98, NO. s1, (78-87), Online publication date: 1-Sep-2006. Michel M and Vrydag W (2009) α 1 -, α 2 - and β-adrenoceptors in the urinary bladder, urethra and prostate British Journal of Pharmacology, 10.1038/sj.bjp.0706619, VOL. 147, NO. S2, (S88-S119), Online publication date: 1-Feb-2006. Yamanishi T, Yasuda K, Kitahara S, Nakai H, Yoshida K and Iizuka H (2006) Effects of 138–355, a β3-adrenoceptor selective agonist, on relaxation of the human detrusor muscle in vitroNeurourology and Urodynamics, 10.1002/nau.20231, VOL. 25, NO. 7, (815-819), . Andersson K and Arner A (2004) Urinary Bladder Contraction and Relaxation: Physiology and PathophysiologyPhysiological Reviews, 10.1152/physrev.00038.2003, VOL. 84, NO. 3, (935-986), Online publication date: 1-Jul-2004. YAMANISHI T, CHAPPLE C, YASUDA K, YOSHIDA K and CHESS-WILLIAMS R (2018) The Functional Role of β-Adrenoceptor Subtypes in Mediating Relaxation of Pig Urethral Smooth MuscleJournal of Urology, VOL. 170, NO. 6, (2508-2511), Online publication date: 1-Dec-2003. Yamanishi T, Chapple C, Yasuda K, Yoshida K and Chess-Williams R (2003) Role of ?-adrenoceptor subtypes in mediating relaxation of the pig bladder trigonal muscle in vitroNeurourology and Urodynamics, 10.1002/nau.10130, VOL. 22, NO. 4, (338-342), . Volume 168Issue 6December 2002Page: 2706-2710 Advertisement Copyright & Permissions© 2002 by American Urological Association, Inc.Keywordsreceptors, adrenergic, betaswineurethrabladderurinary tractMetricsAuthor Information TOMONORI YAMANISHI More articles by this author CHRISTOPHER R. CHAPPLE More articles by this author KOSAKU YASUDA More articles by this author KEN-ICHIRO YOSHIDA More articles by this author RUSSELL CHESS-WILLIAMS More articles by this author Expand All Advertisement PDF downloadLoading ..." @default.
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