| Bioactivity | SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2]. |
| Target | IC50: 40 nM (β3 receptor), 408 nM ((β1 receptor), 648 nM (β2 receptor) |
| Invitro | SR59230A (100 nM-50 μM; 24 hours) is able to reduce cell viability in a dose-dependent manner in Neuro-2A, BE(2)C and SK-N-BE(2) NB cell lines[3]. Cell Viability Assay[3] Cell Line: |
| In Vivo | MDMA (20 mg/kg) produces a slowly developing hyperthermia, reaching a maximum increase of 1.8°C at 130 min post injection. SR59230A (0.5 mg/kg) produces a small but significant attenuation of the slowly developing hyperthermia to MDMA. SR59230A (5 mg/kg) reveals a significant and marked early hypothermic reaction to MDMA[4]. Animal Model: |
| Name | SR59230A hydrochloride |
| CAS | 1135278-41-9 |
| Formula | C21H28ClNO2 |
| Molar Mass | 361.91 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Nisoli E, et al. Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes.Mol Pharmacol. 1996 Jan;49(1):7-14. [2]. Kanzler SA, et al. Involvement of β3-adrenergic receptors in the control of food intake in rats.Braz J Med Biol Res. 2011 Nov;44(11):1141-7. [3]. Bruno G, et al. β3-adrenoreceptor blockade reduces tumor growth and increases neuronal differentiation in neuroblastoma via SK2/S1P2 modulation.Oncogene. 2020 Jan;39(2):368-384. [4]. Bexis S, et al. Role of alpha 1- and beta 3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse. Br J Pharmacol. 2009 Sep;158(1):259-66. |