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HomeProduct name listEFAROXAN HYDROCHLORIDE

EFAROXAN HYDROCHLORIDE

Synonym(s):2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran hydrochloride;RX 821037A

EFAROXAN HYDROCHLORIDE Structural

What is EFAROXAN HYDROCHLORIDE?

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

The Uses of EFAROXAN HYDROCHLORIDE

Efaroxan Hydrochloride is a potent α2-AR adrenoceptor antagonist.

What are the applications of Application

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

Properties of EFAROXAN HYDROCHLORIDE

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 for EFAROXAN HYDROCHLORIDE

Signal word Danger
Pictogram(s)
ghs
Skull and Crossbones
Acute Toxicity
GHS06
GHS Hazard Statements H301:Acute toxicity,oral
Precautionary Statement Codes P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Computed Descriptors for EFAROXAN HYDROCHLORIDE

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