Mirabegron - CAS 223673-61-8
Catalog number:
223673-61-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Adrenergic Receptor
Description:
Mirabegron (formerly YM-178, trade name Myrbetriq) is a drug for the treatment of overactive bladder. It was developed by Astellas Pharma and was approved in the United States in July 2012. Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity
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Purity:
0.99
Synonyms:
YM-178; YM 178; YM178
MSDS:
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1. Pharmacological profile of the selective β3-adrenoceptor agonist mirabegron in cynomolgus monkeys
Toshiki Hatanaka & Masashi Ukai & Mai Watanabe. Naunyn-Schmiedeberg's Arch Pharmacol (2013) 386:1001–1008
Mirabegron is the first β3-adrenoceptor agonist with better balance between efficacy and tolerability for the treatment of overactive bladder compared with existing antimuscarinic agents and has been launched in Japan, the USA, and European countries. We previously reported that mirabegron shows relaxant effects on rats and humans bladder smooth muscle strips in vitro (Takasu et al. 2007; Hatanaka et al. 2013a) and ameliorates effects in rat models of overactive bladder (Hatanaka et al. 2013a) and bladder outlet obstruction (Hatanaka et al. 2013b).
2. β3-Adrenoceptor agonist mirabegron is effective for overactive bladder that is unresponsive to antimuscarinic treatment or is related to benign prostatic hyperplasia in men
Hideo Otsuki • Takeo Kosaka • Kenzo Nakamura. Int Urol Nephrol (2013) 45:53–60
Since it was revealed that β3-adrenoceptor acts as a subtype of relaxation of detrusor, β3-adrenoceptor is considered to be one of the targets of OAB pharmacotherapy. Another action of β3-adrenoceptor agonist is to enhance the storage function of the bladder with less effect on detrusor pressure during micturition and post-void residual urine volume. As a result, mirabegron improves urinary urgency, frequency, and urgency incontinence. The usefulness of β3-adrenoceptor agonist was verified both in vitro and in vivo. Mirabegron appeared on the Japanese market in September 2011, and it provides a new treatment option for OAB.
3. The efficacy and safety of mirabegron in treating OAB: a systematic review and meta-analysis of phase III trials
Yuanshan Cui • Huantao Zong. Int Urol Nephrol (2014) 46:275–284
Mirabegron, a selective β3-adrenoceptor (AR) agonist, is a first in class drug for the treatment of OAB. β3-ARs account for more than 95 % of all b-AR mRNA in the human bladder and are thought to be the main β-ARs mediating human detrusor relaxation. β3-ARs have been found to be highly and preferentially expressed on urinary bladder tissues, including the urothelium, interstitial cells and detrusor smooth muscle, suggesting mirabegron as a new effective and well-tolerated class of drug for patient with OAB symptoms.
4. Mirabegron for Male Lower Urinary Tract Symptoms
Oscar Suarez & David Osborn & Melissa Kaufman. Curr Urol Rep (2013) 14:580–584
Nitti et al enrolled 1,329 patients (24 % male) with OAB and randomly assigned them to one of three treatment arms: placebo, mirabegron 50 mg and mirabegron 100 mg for 12 weeks [19•]. Mirabegron was well tolerated and showed statistically significant reductions in the number of incontinence episodes and in the number of micturitions per 24-h period compared with placebo. Khullar et al carried out a similar randomized European-Australian multicenter trial in which they enrolled 1,978 patients (28 % male) with OAB [20]. In this study, after a 2-week placebo run-in period, patients were randomized to receive placebo, mirabegron 50 mg, mirabegron 100 mg or the active control, tolterodine ER, for 12 weeks. When compared to placebo, mirabegron demonstrated a statistically significant decrease from baseline in mean number of micturitions and mean number of incontinence episodes per 24-h period. Both doses of mirabegron were effective in improving co-primary efficacy endpoints versus placebo.
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CAS 223673-61-8 Mirabegron

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