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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.
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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.
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
Keywords: Efaroxan hydrochloride, Efaroxan hydrochloride supplier, α2-adrenoceptor, alpha2-adrenoceptor, a2-adrenoceptor, α2-Adrenergic, alpha2-Adrenergic, a2-adrenergic, antagonists, I1, I3, ligand, Receptors, General, Imidazolines, Adrenergic, Alpha-2, 0792, Tocris Bioscience
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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.
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