SR-59230A is a potent and selective β3 adrenoceptor antagonist (IC50 values are 40, 408 and 648 nM for β3, β1 and β2 receptors respectively). SR-59230A was subsequently shown to also act at α1 adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies. SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism
Chemical Formula: C23H29NO6
Molecular Weight: 415.486
Elemental Analysis: C, 66.49; H, 7.04; N, 3.37; O, 23.10
Chemical Name: 1-(2-Ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol oxalate
InChi Code: InChI=1S/C21H27NO2.C2H2O4/c1-2-16-8-4-6-13-21(16)24-15-18(23)14-22-20-12-7-10-17-9-3-5-11-19(17)20;3-1(4)2(5)6/h3-6,8-9,11,13,18,20,22-23H,2,7,10,12,14-15H2,1H3;(H,3,4)(H,5,6)/t18-,20-;/m0./s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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.
Jing JN, Li FL, Wang X, Wan X, Zhao QQ, Cui XL. [SR 59230A on the expression of MicroRNAs in myocardium of heart failure rats]. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2017 May 8;33(5):456-460. Chinese. doi: 10.12047/j.cjap.5561.2017.109. PMID: 29926593.
Kulzer M, Seyler C, Welke F, Scherer D, Xynogalos P, Scholz EP, Thomas D, Becker R, Karle CA, Katus HA, Zitron E. Inhibition of cardiac Kir2.1-2.3 channels by beta3 adrenoreceptor antagonist SR 59230A. Biochem Biophys Res Commun. 2012 Jul 27;424(2):315-20. doi: 10.1016/j.bbrc.2012.06.114. Epub 2012 Jun 27. PMID: 22749993.
Pettersson US, Henriksnäs J, Jansson L. Reversal of high pancreatic islet and white adipose tissue blood flow in type 2 diabetic GK rats by administration of the beta3-adrenoceptor inhibitor SR-59230A. Am J Physiol Endocrinol Metab. 2009 Aug;297(2):E490-4. doi: 10.1152/ajpendo.00140.2009. Epub 2009 Jun 2. PMID: 19491297.
Leblais V, Pourageaud F, Ivorra MD, Guibert C, Marthan R, Muller B. Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A, on the contraction of rat intrapulmonary artery. J Pharmacol Exp Ther. 2004 Apr;309(1):137-45. doi: 10.1124/jpet.103.061192. Epub 2004 Jan 12. PMID: 14718590.
MacDonald A, Watt K. Characterisation of the atypical beta-adrenoceptor in rabbit isolated jejunum using BRL 37344, cyanopindolol and SR 59230A. J Auton Pharmacol. 1999 Apr;19(2):91-5. doi: 10.1046/j.1365-2680.1999.00121.x. PMID: 10466941.
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