Catalog No.S4009 Synonyms: YM 178
Molecular Weight(MW): 396.51
Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
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|Description||Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.|
Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron has little agonistic effect on 1- and 2-ARs. Mirabegron concentration-dependently relaxes rat and Human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol with EC50 values of 5.1 μM and 0.78 μM, respectively. The maximal relaxant effects of Mirabegron are 94.0 % and 89.4% that of carbachol, respectively.  Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH as the IC50 value in human liver microsomes decreased from 13 to 4.3 μM after 30 min preincubation. Mirabegron acts partly as an irreversible or quasi-irreversible metabolism-dependent inhibitor of CYP2D6. 
|In vivo||Mirabegron produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. 3 mg/kg i.v. Mirabegron suppresses the frequency to 2 counts/10 min. Mirabegron does not decrease the amplitude of rhythmic bladder contraction.  Mirabegron decreases primary bladder afferent activity and bladder microcontractions in rats. Mirabegron (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling. SAAs of C-fibers decrease only at 1 mg/kg Mirabegron treatment. Mirabegron administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder.  Mirabegron is efficient on facilitation of bladder storage. Mirabegron dose-dependently decreases the resting intravesical pressure. Mirabegron dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. Mirabegron exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity. |
|In vitro||DMSO||79 mg/mL (199.23 mM)|
|Ethanol||8 mg/mL (20.17 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03049462||Recruiting||Healthy Volunteers||National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC)||January 30, 2017||Phase 1|
|NCT02981459||Not yet recruiting||Urinary Frequency/Urgency|Bladder Irritable|Bladder Pain Syndrome||State University of New York at Buffalo|Astellas Pharma Inc||January 2017||Phase 4|
|NCT02279615||Not yet recruiting||Overactive Bladder|Benign Prostatic Hyperplasia||St. Josephs Healthcare Hamilton||December 2016||Phase 4|
|NCT02893553||Recruiting||Spinal Cord Injury|Autonomic Dysreflexia|Baroreceptor Integrity|Sympathetic Integrity|Vagal Integrity|Autonomic Integrity|Hypotensive|Cognitive Function|Cerebral Blood Flow|Blood Pressure||James J. Peters Veterans Affairs Medical Center|Kessler Foundation||December 2016||Phase 2|
|NCT02744430||Not yet recruiting||Ureteral Obstruction|Flank Pain||Baylor College of Medicine||November 2016||Phase 2|
|NCT02916693||Not yet recruiting||Erectile Dysfunction|Overactive Bladder|Urinary Incontinence||Johns Hopkins University|Astellas Pharma US, Inc.||September 2016||Phase 1|Phase 2|
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