1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. SR59230A hydrochloride

SR59230A hydrochloride 

Cat. No.: HY-103200
Handling Instructions

SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

For research use only. We do not sell to patients.

SR59230A hydrochloride Chemical Structure

SR59230A hydrochloride Chemical Structure

CAS No. : 1135278-41-9

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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].

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].

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.
Molecular Weight

361.91

Formula

C₂₁H₂₈ClNO₂

CAS No.

1135278-41-9

SMILES

O[[email protected]@H](CN[[email protected]]1CCCC2=C1C=CC=C2)COC3=CC=CC=C3CC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SR59230AAdrenergic ReceptorBeta Receptorhyperthermiahypothermiaα1adrenoceptorβ3adrenergicreceptorInhibitorinhibitorinhibit

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SR59230A hydrochloride
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HY-103200
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