Mirabegron is for the treatment of urgency, urinary frequency, and urinary urge urinary incontinence associated with overactive bladder (OAB). Mirabegron is synthesized by coupling 4-nitrophenethyl amine to (R)-2-hydroxy-2-phenylacetic acid. The resulting amide is reduced to an amine. The nitro group is then reduced and the resulting is coupled to 2-(2-aminothiazol-4-yl) acetic acid to give mirabegron. Mirabegron has an EC50 of 22 nM (intrinsic activity=0.8) for β3-AR with no detectable activity for β1- andβ2-AR (EC50>10,000 nM). In an anesthetized rat rhythmic bladder contraction model in which bladder contractions are induced by saline, mirabegron at 3 mg/kg iv decreased the frequency of rhythmic bladder contraction without suppressing contraction amplitude. These data suggest that the activation of β3-AR increases bladder capacity without influencing the frequency of bladder contraction.
Function and Application
1.Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
2.Uses for A potent bladder relaxant compound
3.Uses for Potent bladder relaxant and reagent for diabetes remedy.;Labeled Mirabegron, intended for use as an internal standard for the quantification of Mirabegron by GC- or LC-mass spectrometry.
White or off-white crystalline powder
Off-white crystalline powder
1)The infrared absorption spectrum is in accordance with the spectrum obtained with Mirabegron RS.
2)The retention time of the major peak in the chromatogram obtained with test solution conform to that in the chromatogram obtained with reference solution as Assay test.