[CAS NO. 1135278-41-9] SR59230A hydrochloride
PRODUCTS SPECIFICATIONS [1135278-41-9]
DESCRIPTION [1135278-41-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 361.91 |
| Molecular Formula | C21H28ClNO2 |
| SMILES | O[C@@H](CN[C@H]1CCCC2=C1C=CC=C2)COC3=CC=CC=C3CC.[H]Cl |
5 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 40 nM (β3 receptor), 408 nM ((β1 receptor), 648 nM (β2 receptor) [2]
In Vitro
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [3]
| Cell Line: | Three different neuroblastoma (NB) cell lines, one murine (Neuro-2A) and two human (SK-N-BE(2), BE(2)C) |
| Concentration: | 100 nM, 1 μM, 5 μM, 10 μM, and 50 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced cell viability in a dose-dependent manner, with significant effect at a concentration limit over 1 µM for Neuro-2A cells and 5 µM for SK-N-BE(2) and BE(2)C). |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male C-57BL6J wild-type mice (22-35 g) [4] |
| Dosage: | 0.5 or 5 mg/kg |
| Administration: | Injected s.c.; administered 30 min prior to the injection s.c. of MDMA (20 mg/kg). |
| Result: | Modulated the actions of MDMA on temperature involve α1-adrenoceptor antagonism. |
Appearance
Solid
Shipping
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)
Solvent & Solubility
DMSO : 250 mg/mL ( 690.78 mM ; Need ultrasonic)
H 2 O : 2.5 mg/mL ( 6.91 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7631 mL | 13.8156 mL | 27.6312 mL |
| 5 mM | 0.5526 mL | 2.7631 mL | 5.5262 mL |
| 10 mM | 0.2763 mL | 1.3816 mL | 2.7631 mL |
References
- [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.