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Overview
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Background
SR 59230A hydrochloride is a selective and potent antagonist of β3 adrenoceptor, with IC50 values being 40, 408, and 648 nM for β3, β1, and β2 adrenergic receptors, respectively. β3 adrenoceptor, predominately located in adipose tissue, is mainly responsible for the regulation of lipolysis and thermogenesis. In addition, β3 adrenoceptor has also been found to be involved in different tumor conditions, such as neuroblastoma, via the regulation of the bioactive lipid sphingosine 1-phosphate metabolism and signaling.
1. Nisoli E, Tonello C, Landi M, et al. Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes. Molecular Pharmacology, 1996, 49(1): 7-14.
2. Kanzler SA, Januario AC, Paschoalini MA. Involvement of β3-adrenergic receptors in the control of food intake in rats. Brazilian Journal of Medical and Biological Research, 2011, 44(11): 1141-1147.
3. Bruno G, Cencetti F, Pini A, et al. β3-adrenoreceptor blockade reduces tumor growth and increases neuronal differentiation in neuroblastoma via SK2/S1P2 modulation. Oncogene, 2020, 39(2): 368-384.
4. Bexis S, Docherty JR. Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse. British Journal of Pharmacology, 2009, 158(1): 259-266.
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