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  • Title: An aryloxypropanolamine hβ3-adrenoceptor agonist as bladder smooth muscle relaxant.
    Author: Tasler S, Baumgartner R, Behr-Roussel D, Oger-Roussel S, Gorny D, Giuliano F, Ney P.
    Journal: Eur J Pharm Sci; 2012 Aug 15; 46(5):381-7. PubMed ID: 22430195.
    Abstract:
    The relaxant effect of an aryloxypropanolamine β3-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 hβ3-AR agonists have been evaluated and discussed thoroughly. A ranking of hβ3-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.
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