SR59230A

Modify Date: 2025-08-25 11:09:43

SR59230A Structure
SR59230A structure
Common Name SR59230A
CAS Number 174689-39-5 Molecular Weight 415.47900
Density N/A Boiling Point 542.6ºC at 760mmHg
Molecular Formula C23H29NO6 Melting Point N/A
MSDS USA Flash Point 281.9ºC

 Use of SR59230A


SR59230A 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].

 Names

Name SR 59230A hydrochloride,1-(2-Ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanolhydrochloride
Synonym More Synonyms

 SR59230A Biological Activity

Description SR59230A 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].
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

[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.

 Chemical & Physical Properties

Boiling Point 542.6ºC at 760mmHg
Molecular Formula C23H29NO6
Molecular Weight 415.47900
Flash Point 281.9ºC
Exact Mass 415.19900
PSA 116.09000
LogP 3.20240
Vapour Pressure 1.27E-11mmHg at 25°C

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Risk Phrases 22-24/25
RIDADR NONH for all modes of transport

 Articles6

More Articles
Functional evidence of atypical beta 3-adrenoceptors in the human colon using the beta 3-selective adrenoceptor antagonist, SR 59230A.

Br. J. Pharmacol. 117(7) , 1374-6, (1996)

The role of beta 3-adrenoceptors in human colonic circular smooth muscle was assessed in vitro by use of the beta 3-selective antagonist SR 59230A. Isoprenaline, in the presence of the selective beta-...

ALpha1-adrenoceptor antagonist properties of CGP 12177A and other beta-adrenoceptor ligands: evidence against beta(3)- or atypical beta-adrenoceptors in rat aorta.

Br. J. Pharmacol. 142 , 781-787, (2004)

1. The alpha(1)-adrenoceptor antagonist properties of the beta-adrenoceptor nonconventional partial agonist, CGP 12177A, was investigated in functional assays in rat aorta and in radioligand binding a...

Costunolide and Dehydrocostuslactone, two natural sesquiterpene lactones, ameliorate the inflammatory process associated to experimental pleurisy in mice.

Eur. J. Pharmacol. 730 , 107-15, (2014)

The aim of this study was to investigate the effect of costunolide (CS) and dehydrocostuslactone (DCE) a well-known sesquiterpene lactones contained in many plants, in a model of lung injury induced b...

 Synonyms

3-(2-Ethylphenoxy)-1-[[(1S)-1,2,3,4-tetrahydronaphth-1-yl]amino]-(2S)-2-propanol oxalate salt
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