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Efaroxan hydrochloride

Product NameEfaroxan hydrochloride
CAS89197-00-2
MFC13H17ClN2O
MW252.74
EINECS
MOL File89197-00-2.mol

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.
InChI	InChI=1S/C13H16N2O.ClH/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13;/h3-6H,2,7-9H2,1H3,(H,14,15);1H
InChIKey	DWOIUCRHVWIHAH-UHFFFAOYSA-N
SMILES	C(C1(C2NCCN=2)OC2C=CC=CC=2C1)C.Cl

Safety Information

Hazard Codes	T
Risk Statements	25
Safety Statements	7-35-45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
Storage Class	6.1C - Combustible acute toxic Cat.3 toxic compounds or compounds which causing chronic effects
Hazard Classifications	Acute Tox. 3 Oral

MSDS

Provider	Language
SigmaAldrich	English

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 .

in vivo

Efaroxan hydrochloride increases plasma insulin levels in both conscious fed and fasted rats without greatly affecting plasma glucoselevels^[3].

Animal Model:	Male Sprague-Dawley rats (weight range 250-300g)^[3]
Dosage:	1 mg/kg, 5 mg/kg
Administration:	Oral administration
Result:	Produced a significant increase in plasma insulin levels of starved rats 15 and 30 min after treatment.

IC 50

α adrenergic receptor

References

[1] CHRISTOPHER B. CHAPLEO. .alpha.-Adrenoceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on .alpha.-adrenoreceptor activity[J]. Journal of Medicinal Chemistry, 1984, 27 5: 570-576. DOI:10.1021/jm00371a003
[2] R M EGLEN. “Seeing through a glass darkly”: casting light on imidazoline “I” sites.[J]. Trends in pharmacological sciences, 1998, 19 9: 381-390. DOI:10.1016/s0165-6147(98)01244-9
[3] GABRIEL OLMOS . Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors[J]. European journal of pharmacology, 1994, 262 1: Pages 41-48. DOI:10.1016/0014-2999(94)90026-4
[4] TIMOTHY L. BERRIDGE Alan G R John C Doxey. Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats[J]. European journal of pharmacology, 1992, 213 2: Pages 213-218. DOI:10.1016/0014-2999(92)90684-v

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