Efaroxan HCl
α2 adrenergic antagonist / Selective α2-adrenergic receptor antagonist1 (selectivity ratio of α2/α1 = 724)4 and imidazoline receptor antagonist2. Induces release of insulin in the rat insulinoma cell line RIN-5AH by interaction with ATP-sensitive potassium channels independently from imidazoline I1 or I2 receptors.3 Increases resting plasma insulin levels and markedly potentiates the rise in insulin levels produced by adrenaline in the rat.4
Biochemicals & reagents
89197-00-2
RX 821037A
1) Chapleo et al. (1984), alpha-Adrenoceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoceptor activity; J.Med.Chem., 27 570 2) Eglen et al. (1998), ‘Seeing through a glass darkly’: casting light on imidazoline ‘I’ sites; Trends Pharmacol.Sci. 19 381 3) 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 4) Berridge et al. (1992), Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats; Eur.J.Pharmacol. 213 205
-20°C
TARGET: GPCR -- PATHWAY: Ion channels -- DISEASE AREA: Diabetes