SR59230A

A β3-AR antagonist

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库存: 现货

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5mg

￥1412.00

1130.00

- +
10mg

￥2400.00

1920.00

- +
50mg

￥8637.00

6910.00

- +

已选 0 种 0 瓶

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Background

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 (K_is = 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 G_s pathway.⁴ It has also been used in studies of heart failure to elucidate the role of the β₃-ARs.⁵

1.Manara, L., Badone, D., Baroni, M., et al.Functional identification of rat atypical β-adrenoceptors by the first β3-selective antagonists, aryloxypropanolaminotetralinsBr. 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 cellsNaunyn-Schmiedeberg's 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 mouseBr. 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 adipocytesBr. 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 failureChin. Med. J. (Engl.)120(24)2250-2255(2007)