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Efaroxan HCl | α2 adrenergic antagonist

CAS:
89197-00-2
Catalog Number:
10-1342
Activity:
α2 adrenergic antagonist
Alternate Names:
RX 821037A
Chemical Name:
2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran, hydrochloride
Molecular Weight:
252.74
Molecular Formula:
C13H16N2O HCl
Solubility:
Soluble in Water (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
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.
Shipping Code:
RT

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

References/Citations:

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

Efaroxan HCl | α2 adrenergic antagonist is also available in the Cellular Metabolism Library.
CAS:
89197-00-2
Catalog Number:
10-1342
Activity:
α2 adrenergic antagonist
Alternate Names:
RX 821037A
Chemical Name:
2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran, hydrochloride
Molecular Weight:
252.74
Molecular Formula:
C13H16N2O HCl
Solubility:
Soluble in Water (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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