EFAROXAN HYDROCHLORIDE
Synonym(s):2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran hydrochloride;RX 821037A
- CAS NO.:89197-00-2
- Empirical Formula: C13H17ClN2O
- Molecular Weight: 252.74
- MDL number: MFCD00069270
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-08 09:03:00
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) |
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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