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Efaroxan hydrochloride
Chemical Name:2-(2-Ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-i
midazole hydrochloride
Biological Activity:
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 α2A, 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.
Chapleoet 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. Olmoset al (1994) Imidazolines stimulate release of insulin
from RIN-5AH cells independently from imidazoline I1 and I2
receptors. Eur.J.Pharmacol. 262 41. Eglen et al (1998)
'Seeing through a glass darkly': casting light on imidazoline 'I' sites. TiPS 19
381. Mayer and Taberner (2002) Effects of the imidazoline ligands
efaroxan and KU14R on blood glucose in the mouse. Eur.J.Pharmacol. 454
95.
