Name | SR 59230A hydrochloride |
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Synonyms |
2-Propanol, 1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-, (2S)-, hydrochloride (1:1)
(2S)-1-(2-Ethylphenoxy)-3-[(1S)-1,2,3,4-tetrahydronaphthalen-1-ylamino]propan-2-ol hydrochloride (1:1) (2S)-1-(2-Ethylphenoxy)-3-[(1S)-1,2,3,4-tetrahydro-1-naphthalenylamino]-2-propanol hydrochloride (1:1) |
Description | 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]. |
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Related Catalog | |
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]. 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]. 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. |
References |
Molecular Formula | C21H28ClNO2 |
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Molecular Weight | 361.905 |
Exact Mass | 361.180847 |
Appearance | off-white solid |
Storage condition | store at -20℃ for one year(Powder) |
Water Solubility | Soluble in water (10 mM), and DMSO (100 mM). |