An aryloxypropanolamine h尾3-adrenoceptor agonist as bladder smooth muscle relaxant

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• 作者：Stefan Tasler^a ; ^{stefan.tasler@4sc.com} ; Roland Baumgartner^a ; Delphine Behr-Roussel^b ; ^c ; Stephanie Oger-Roussel^b ; ^c ; Diane Gorny^b ; ^c ; Francois Giuliano^c ; Peter Ney^d
• 关键词：AR ; adrenergic receptor ; CCh ; carbachol ; FSK ; forskolin ; PBS ; phosphate-buffered saline
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2012
• 期刊代码：15_09280987
• 类别：pha
• 出版时间：15 August, 2012
• 卷：46
• 期：5
• 页码：381-387
• 文件大小：369 K

摘要

The relaxant effect of an aryloxypropanolamine 尾3-adrenoceptor agonist on carbachol pre-contracted human detrusor muscle strips was evaluated and compared with literature results from reference compounds of similar mode of action, including mirabegron. A significant relaxation was observed for rac-4-{2-hydroxy-3-[1-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-ylamino]propoxy}-2-(hydroxymethyl)phenol which was similar to that exerted by mirabegron. In order to allow for a thorough discussion of results in comparison to reference compounds, their affinity, selectivity and efficacy as h尾3-AR agonists have been evaluated and discussed thoroughly. A ranking of h尾3-AR agonists by relative efficacy resulted in the closest analogy to the order of relaxation potential, with only the relaxant effect of mirabegron not reflecting its excellent relative efficacy as such.