EFAROXAN HYDROCHLORIDE Chemical Properties

storage temp. 

Store at RT

solubility 

H₂O: 300 mg/mL

form 

solid

color 

White

Water Solubility 

Soluble to 100 mM in water

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20° for up to 1 month.

Safety Information

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

7-35-45

RIDADR 

UN 2811 6.1/PG 3

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

EFAROXAN HYDROCHLORIDE Usage And Synthesis

Description

Efaroxan HCl (89197-00-2) is a 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 Efaroxan HCl increases resting plasma insulin levels and markedly potentiates the rise in insulin levels produced by adrenaline in the rat.4

Uses

Efaroxan Hydrochloride is a potent α2-AR adrenoceptor antagonist.

Biological Activity

Potent, highly selective α 2 adrenoceptor antagonist and imidazoline I 1 receptor ligand (pK i values are 7.87, 7.42, 5.74, 7.28 and < 5 for α 2A , α 2B , α 2C , I 1 , and I 2 receptors respectively). Promotes insulin secretion, at a site distinct from I 1 or I 2 (the putative I 3 receptor) in vitro and in vivo .

References

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

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