Mirabegron 是选择性的肾上腺素受体激动剂，EC50=22.4 nM。

Mirabegron is a beta-3 adrenergic agonist that is used for treatment of overactive bladder syndrome.

在麻醉大鼠中,静脉注射Mirabegron（3 mg / kg）能够产生降低节律性膀胱收缩频率,但不会影响收缩幅度.

在表达人类3-肾上腺素能受体CHO细胞中,Mirabegron以浓度依赖的方式增加cAMP在细胞内的积累。在用10-6M或10-7M卡巴胆碱预处理的大鼠膀胱平滑肌（EC50=5.1 μM）和人膀胱平滑肌（EC50=0.78 μM）中,Mirabegron能够产生放松作用。

Mirabegron (YM178) is dissolved in 100% DMSO and diluted with assay buffer[1]. CHO cells (105) are seeded in each well of a 24-well culture plate and subcultured. Three days later, the medium is exchanged with 250 μL/well Hanks' balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine, pH 7.4. The cells are incubated with each compound (isoproterenol, Mirabegron, BRL37344, and CL316,243 at final concentrations of 10-10 to 10-4 M) for 10 min at 37°C, after which incubation is stopped by the addition of 250 μL of 0.2 M HCl. cAMP concentration in the reaction mixture is measured by radioimmunoassay using an 125I-cAMP assay system using a gamma counter. Fifty microliters of reaction mixture is incubated with 50 μL of succinyl agent for 10 min at room temperature, after which the reaction is stopped by the addition of 400 μL of buffer solution. Fifty microliters of succinylated sample is incubated with 50 μL of 125I-cAMP and 50 μL of anti-cAMP antibody for 24 h at 4°C. At the end of the incubation period, 250 μL of charcoal suspension is added and centrifuged for 10 min at 2800 g at 4°C. Two hundred and fifty microliters of supernatant is transferred into a tube and counted for 1 min using a gamma counter. The intrinsic activity (I.A.) relative to isoproterenol for each β-adrenoceptor agonist is calculated using the maximal response of each compound[1].

223673-61-8

C21H24N4O2S

396.51

YM178;米拉贝隆

Ethanol:8 mg/mL (20.17 mM)
DMSO:73 mg/mL (184.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years