SR 59230A hydrochloride

R 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.

References:

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.