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Biological Activity for Efaroxan hydrochloride
Efaroxan hydrochloride is a potent, highly selective α2 adrenoceptor antagonist and imidazoline I1 receptor ligand (pKi values are 7.87, 7.42, 5.74, 7.28 and < 5 for α 2A, α2B, α2C, I1, and I2 receptors respectively). Promotes insulin secretion, at a site distinct from I1 or I2 (the putative I3 receptor) in vitro and in vivo.
Technical Data for Efaroxan hydrochloride
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Efaroxan hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Efaroxan hydrochloride
The following data is based on the product molecular weight 252.74. Batch specific molecular weights may vary from batch to batch due to the degree 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||3.96 mL||19.78 mL||39.57 mL|
|5 mM||0.79 mL||3.96 mL||7.91 mL|
|10 mM||0.4 mL||1.98 mL||3.96 mL|
|50 mM||0.08 mL||0.4 mL||0.79 mL|
Product Datasheets for Efaroxan hydrochloride
References for Efaroxan hydrochloride
References are publications that support the biological activity of the product.
Chapleo et al (1984) α-Adrenoceptor reagents 2. Effects of modification of the 1,4-benzodioxan ring system on α-adrenoceptor activity. J.Med.Chem. 27 570 PMID: 6143826
Eglen et al (1998) 'Seeing through a glass darkly': casting light on imidazoline 'I' sites. TiPS 19 381 PMID: 9786027
Mayer and Taberner (2002) Effects of the imidazoline ligands efaroxan and KU14R on blood glucose in the mouse. Eur.J.Pharmacol. 454 95 PMID: 12409010
Olmos et al (1994) Imidazolines stimulate release of Ins from RIN-5AH cells independently from imidazoline I1 and I2 receptors. Eur.J.Pharmacol. 262 41 PMID: 7813577
If you know of a relevant reference for Efaroxan hydrochloride, please let us know.
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Citations for Efaroxan hydrochloride
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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* 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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.