Cat. No. 0792
Chemical Name: 2-(2-Ethyl-2,3-dihydro-2-benzofuran
Biological ActivityPotent, 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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References are publications that support the products' biological activity.
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.
Eglen et al (1998) 'Seeing through a glass darkly': casting light on imidazoline 'I' sites. TiPS 19 381. PMID: 9786027.
Olmos et al (1994) Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors. Eur.J.Pharmacol. 262 41. PMID: 7813577.
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.
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Keywords: Efaroxan hydrochloride, supplier, α2-adrenoceptor, alpha2-adrenoceptor, a2-adrenoceptor, α2-Adrenergic, alpha2-Adrenergic, a2-adrenergic, antagonists, I1, I3, ligand, Receptors, General, Imidazolines, Tocris Bioscience, Adrenergic α2 Receptor Antagonist products