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• W2334284448 abstract "You have accessJournal of UrologyBenign Prostatic Hyperplasia: Basic Research & Pathophysiology1 Apr 2016MP44-13 EFFECTS OF THE RECEPTOR ANTAGONIST PICOTAMIDE ON ENDOTHELIN-1-, -2- AND -3-INDUCED CONTRACTIONS IN HUMAN PROSTATE SMOOTH MUSCLE Alexander Tamalunas, Christian Gratzke, Frank Strittmatter, Raphaela Waidelich, Christian Stief, and Martin Hennenberg Alexander TamalunasAlexander Tamalunas More articles by this author , Christian GratzkeChristian Gratzke More articles by this author , Frank StrittmatterFrank Strittmatter More articles by this author , Raphaela WaidelichRaphaela Waidelich More articles by this author , Christian StiefChristian Stief More articles by this author , and Martin HennenbergMartin Hennenberg More articles by this author View All Author Informationhttps://doi.org/10.1016/j.juro.2016.02.269AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookTwitterLinked InEmail INTRODUCTION AND OBJECTIVES Prostate smooth muscle contraction functions as the dynamic component of lower urinary tract symptoms (LUTS) secondary to benign prostatic enlargement. This is critical for pathophysiology of LUTS, and the main starting point when approaching therapy. The current gold standard are α1-adrenoceptor blockers, although their maximum efficacy is limited to only 50 % improvement. This may be explained by non-adrenergic mediators of contraction contributing to prostate smooth muscle tone, but without being inhibited by a1-blockers. Thus, new medications addressing adrenergic and non-adrenergic contractions at once may be highly attractive. We have recently shown that the receptor antagonist picotamide inhibits α1-adrenergic and thromboxane-induced contractions in the prostate. Here, we addressed effects of picotamide on endothelin-1-, -2-, and -3-induced contractions of human prostate smooth muscle. METHODS Prostate tissues were obtained from patients undergoing radical prostatectomy for prostate cancer (n=19 patients). Tissues were prepared from the periurethral zone to ensure that samples were not infiltrated by cancer. Contractility of prostate strips was then assessed in an organ bath. RESULTS Endothelin-1, -2 and -3 induced concentration-dependent contractions of human prostate tissues. Contractions induced by each of all three endothelins were inhibited by the thromboxane receptor antagonist picotamide (300 µM). For endothelin-1 (n=6 patients), inhibition was significant at 3 µM (p<0.03 vs. control). For endothelin-2 (n=8 patients), inhibition was significant at all concentrations, i. e. at 0.1 µM (p<0.01 vs. control), 0.3 µM (p<0.04), 1 µM (p<0.03), 3 µM (p<0.05). For endothelin-3 (n=5 patients), inhibition was significant at 0.1 µM (p<0.05 vs. control), 0.3 µM (p<0.02), 1 µM (p<0.008) and at 3 µM (p<0.004). CONCLUSIONS Prostate smooth muscle contraction is induced by all three endothelins. These contractions could be inhibited by the receptor antagonist picotamide. Because picotamide interfers with adrenergic and non-adrenergic prostate smooth muscle contraction, it may be superior to α1-blockers. © 2016FiguresReferencesRelatedDetails Volume 195Issue 4SApril 2016Page: e603-e604 Advertisement Copyright & Permissions© 2016MetricsAuthor Information Alexander Tamalunas More articles by this author Christian Gratzke More articles by this author Frank Strittmatter More articles by this author Raphaela Waidelich More articles by this author Christian Stief More articles by this author Martin Hennenberg More articles by this author Expand All Advertisement Advertisement PDF downloadLoading ..." @default.
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• W2334284448 title "MP44-13 EFFECTS OF THE RECEPTOR ANTAGONIST PICOTAMIDE ON ENDOTHELIN-1-, -2- AND -3-INDUCED CONTRACTIONS IN HUMAN PROSTATE SMOOTH MUSCLE" @default.
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