SR 59230A hydrochloride
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.
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.
| Physical Appearance | White solid |
| Storage | Store at RT |
| M.Wt | 361.91 |
| Cas No. | 1135278-41-9 |
| Formula | C21H27NO2·HCl |
| Solubility | Soluble in DMSO |
| Chemical Name | (S)-1-(2-ethylphenoxy)-3-(((S)-1,2,3,4-tetrahydronaphthalen-1-yl)amino)propan-2-ol hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | O[C@H](COC1=CC=CC=C1CC)CN[C@H]2CCCC3=CC=CC=C23.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[3] | |
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Cell lines |
Neuroblastoma cell lines, including murine Neuro-2A, as well as human BE(2)C and SK-N-BE(2) |
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Reaction Conditions |
100 nM ~ 50 μM SR 59230A hydrochloride for 24 h incubation |
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Applications |
SR 59230A hydrochloride was able to reduce cell viability in a dose-dependent manner in Neuro-2A, BE(2)C and SK-N-BE(2) neuroblastoma cell lines. |
| Animal experiment:[4] | |
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Animal models |
Male C-57BL6J wild-type mice, 22-35 g |
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Dosage form |
0.5 or 5 mg/kg Injected subcutaneously 30 min prior to the subcutaneous injection of MDMA |
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Applications |
At a low concentration of 0.5 mg/kg, SR 59230A hydrochloride produced a small but significant attenuation of the slowly developing hyperthermia to methylenedioxymethamphetamine (MDMA). At a high concentration of 5 mg/kg, SR 59230A hydrochloride revealed a significant and marked early hypothermic reaction to MDMA. |
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Note |
The technical data provided above is for reference only. |
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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. |
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Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
