1135278-41-9

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). 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). 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. In adipocytes, it induces phosphorylation of p38 MAPK via the G_s pathway. It has also been used in studies of heart failure to elucidate the role of the β₃-ARs.

SR 59230A Hydrochloride is a potent and selective β3 adrenergic receptor antagonist.

β adrenergic receptor

Store at 4°C

[1] L MANARA. Functional identification of rat atypical beta-adrenoceptors by the first beta 3-selective antagonists, aryloxypropanolaminotetralins.[J]. British Journal of Pharmacology, 1996, 117 3: 435-442. DOI: 10.1111/j.1476-5381.1996.tb15209.x
[2] C HOFFMANN. Comparative pharmacology of human beta-adrenergic receptor subtypes–characterization of stably transfected receptors in CHO cells.[J]. Naunyn-Schmiedeberg’s archives of pharmacology, 2004, 369 2: 151-159. DOI: 10.1007/s00210-003-0860-y
[3] SOTIRIA BEXIS  James R D. Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse[J]. British Journal of Pharmacology, 2009, 158 1: 259-266. DOI: 10.1111/j.1476-5381.2009.00186.x
[4] K. MIZUNO. Stimulation of β3‐adrenoceptors causes phosphorylation of p38 mitogen‐activated protein kinase via a stimulatory G protein‐dependent pathway in 3T3‐L1 adipocytes[J]. British Journal of Pharmacology, 2002, 135 1. DOI: 10.1038/sj.bjp.0704537
[5] RUN-TAO GAN. Chronic blocking of β3-adrenoceptor ameliorates cardiac function in rat model of heart failure[J]. Chinese Medical Journal, 2007, 120 1: 2250-2255. DOI: 10.1097/00029330-200712020-00018