SR 59230A hydrochloride
Potent and selective β3 adrenoceptor antagonist (IC50 values are 40, 408 and 648 nM for β3, β1 and β2 receptors respectively). Orally active in vivo. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 361.91. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.76 mL||13.82 mL||27.63 mL|
|5 mM||0.55 mL||2.76 mL||5.53 mL|
|10 mM||0.28 mL||1.38 mL||2.76 mL|
|50 mM||0.06 mL||0.28 mL||0.55 mL|
References are publications that support the biological activity of the product.
Manara et al (1996) Functional identification of rat atypical β-adrenoceptors by the first β3-selective antagonists, aryloxypropanolaminotetralins. Br.J.Pharmacol. 117 435 PMID: 8821531
Mizuno et al (2002) Stimulation of β3-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytes. Br.J.Pharmacol. 135 951 PMID: 11861323
Manara et al (1995) Aryloxypropanolaminotetralins are the first selective antagonists for atypical (β3) β-adrenoceptors. Pharmacol.Comm. 6 253
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13 Citations for SR 59230A hydrochloride
Citations are publications that use Tocris products. Selected citations for SR 59230A hydrochloride include:
Martínez-Sánchez et al (2017) Hypothalamic AMPK-ER Stress-JNK1 Axis Mediates the Central Actions of Thyroid Hormones on Energy Balance. Cell Metab 26 212 PMID: 28683288
Armaiz-Pena et al (2015) Adrenergic regulation of monocyte chemotactic protein 1 leads to enhanced macrophage recruitment and ovarian carcinoma growth. Oncotarget 6 4266 PMID: 25738355
Lavine (2017) β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression. Invest Ophthalmol Vis Sci 58 299 PMID: 28114591
Brosnahan et al (2013) Norepinephrine potentiates proinflammatory responses of human vaginal epithelial cells. J Neurosci 259 42583 PMID: 23571017
Rankovic et al (2011) Modulation of calcium-dependent inactivation of L-type Ca2+ channels via β-adrenergic signaling in thalamocortical relay neurons. PLoS One 6 e27474 PMID: 22164209
Enriori et al (2011) Leptin action in the dorsomedial hypothalamus increases sympathetic tone to brown adipose tissue in spite of systemic leptin resistance. Mamm Genome 31 12189 PMID: 21865462
Nackley et al (2007) Catechol-O-methyltransferase inhibition increases pain sensitivity through activation of both beta2- and beta3-adrenergic receptors. Pain 128 199 PMID: 17084978
Maupoil et al (2007) Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors. Br J Pharmacol 150 899 PMID: 17325650
Sun et al (2015) Adrenergic DNA damage of embryonic pluripotent cells via β2 receptor signalling. J Neuroimmunol 5 15950 PMID: 26516061
Sood et al (2010) Adrenergic modulation of focal adhesion kinase protects human ovarian cancer cells from anoikis. J Clin Invest 120 1515 PMID: 20389021
Lavine et al (2013) Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol 131 376 PMID: 23303344
Ataka et al (2013) Bone marrow-derived microglia infiltrate into the paraventricular nucleus of chronic psychological stress-loaded mice. PLoS One 8 e81744 PMID: 24303068
Cirino et al (2003) Involvement of β 3-adrenergic receptor activation via cyclic GMP- but not NO-dependent mechanisms in human corpus cavernosum function. Sci Rep 100 5531 PMID: 12707413
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.