| dc.date | 2016 | |
| dc.date | 2016-06-03T20:12:03Z | |
| dc.date | 2016-06-03T20:12:03Z | |
| dc.date.accessioned | 2018-03-29T01:31:19Z | |
| dc.date.available | 2018-03-29T01:31:19Z | |
| dc.identifier | | |
| dc.identifier | British Journal Of Pharmacology. John Wiley And Sons Inc., v. 173, n. 3, p. 415 - 428, 2016. | |
| dc.identifier | 71188 | |
| dc.identifier | 10.1111/bph.13367 | |
| dc.identifier | http://www.scopus.com/inward/record.url?eid=2-s2.0-84956726880&partnerID=40&md5=7a681af573c11c633ce2eb5435235457 | |
| dc.identifier | http://repositorio.unicamp.br/jspui/handle/REPOSIP/237746 | |
| dc.identifier | 2-s2.0-84956726880 | |
| dc.identifier.uri | http://repositorioslatinoamericanos.uchile.cl/handle/2250/1304407 | |
| dc.description | Background and Purpose Mirabegron is the first β3-adrenoceptor agonist approved for treatment of overactive bladder syndrome. This study aimed to investigate the effects of β3-adrenoceptor agonist mirabegron in mouse urethra. The possibility that mirabegron also exerts α1-adrenoceptor antagonism was also tested in rat smooth muscle preparations presenting α1A- (vas deferens and prostate), α1D- (aorta) and α1B-adrenoceptors (spleen). Experimental Approach Functional assays were carried out in mouse and rat isolated tissues. Competition assays for the specific binding of [3H]prazosin to membrane preparations of HEK-293 cells expressing each of the human α1-adrenoceptors, as well as β-adrenoceptor mRNA expression and cyclic AMP measurements in mouse urethra, were performed. Key Results Mirabegron produced concentration-dependent urethral relaxations that were shifted to the right by the selective β3-adrenoceptor antagonist L-748,337 but unaffected by β1- and β2-adrenoceptor antagonists (atenolol and ICI-118,551 respectively). Mirabegron-induced relaxations were enhanced by the PDE4 inhibitor rolipram, and the agonist stimulated cAMP synthesis. Mirabegron also produced rightward shifts in urethral contractions induced by the α1-adrenoceptor agonist phenylephrine. Schild regression analysis revealed that mirabegron behaves as a competitive antagonist of α1-adrenoceptors in urethra, vas deferens and prostate (α1A-adrenoceptor, pA2 ≃ 5.6) and aorta (α1D-adrenoceptor, pA2 ≃ 5.4) but not in spleen (α1B-adrenoceptor). The affinities estimated for mirabegron in functional assays were consistent with those estimated in radioligand binding with human recombinant α1A- and α1D-adrenoceptors (pKi ≃ 6.0). Conclusion and Implications The effects of mirabegron in urethral smooth muscle are the result of β3-adrenoceptor agonism together with α1A and α1D-adrenoceptor antagonism. © 2015 The British Pharmacological Society. | |
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| dc.language | en | |
| dc.publisher | John Wiley and Sons Inc. | |
| dc.relation | British Journal of Pharmacology | |
| dc.rights | fechado | |
| dc.source | Scopus | |
| dc.title | Mirabegron Relaxes Urethral Smooth Muscle By A Dual Mechanism Involving β3-adrenoceptor Activation And α1-adrenoceptor Blockade | |
| dc.type | Artículos de revistas | |
