| 货号 | 21407-1mg |
| 描述 | SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).1 It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).2 At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.3 In adipocytes, it induces phosphorylation of p38 MAPK via the Gspathway.4 It has also been used in studies of heart failure to elucidate the role of the β3-ARs.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Manara, L.,Badone, D.,Baroni, M., et al. Functional identification of rat atypical β-adrenoceptors by the first β3-selective antagonists, aryloxypropanolaminotetralins. Br. J. Pharmacol. 117(3), 435-442 (1996). 2.Hoffman, C.,Leitz, M.R.,Oberdorf-Maass, S., et al. Comparative pharmacology of human β-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn-Schmiedebergs Arch. Pharmacol. 369(2), 151-159 (2004). 3.Bexis, S., and Docherty, J.R. Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse. Br. J. Pharmacol. 158(1), 259-266 (2009). 4.Mizuno, K.,Kanda, Y.,Kuroki, Y., et al. Stimulation of β3-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytes. Br. J. Pharmacol. 135(4), 951-960 (2002). 5.Gan, R.T.,Li, W.M.,Xiu, C.H., et al. Chronic blocking of β3-adrenoceptor ameliorates cardiac function in rat model of heart failure. Chin. Med. J. (Engl.) 120(24), 2250-2255 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | 22 |
| 纯度 | ≥99% |
| 计算分子量 | 361.9 |
| 分子式 | C21H27NO2 • HCl |
| CAS号 | 1135278-41-9 |
| 稳定性 | ≥ 1 year |
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