Efaroxan hydrochloride

Modify Date: 2024-01-02 11:57:21

Efaroxan hydrochloride Structure
Efaroxan hydrochloride structure
Common Name Efaroxan hydrochloride
CAS Number 89197-00-2 Molecular Weight 252.740
Density N/A Boiling Point 387ºC at 760 mmHg
Molecular Formula C13H17ClN2O Melting Point N/A
MSDS Chinese USA Flash Point 187.9ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of Efaroxan hydrochloride


Efaroxan hydrochloride is a potent and selective α2-adrenoceptor antagonist, antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist and can be used for the research of cardiovascular disease[1][2][3].

 Names

Name 2-(2-ethyl-3H-1-benzofuran-2-yl)-4,5-dihydro-1H-imidazole,hydrochloride
Synonym More Synonyms

 Efaroxan hydrochloride Biological Activity

Description Efaroxan hydrochloride is a potent and selective α2-adrenoceptor antagonist, antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist and can be used for the research of cardiovascular disease[1][2][3].
Related Catalog
Target

α2-adrenoceptor, I1-Imidazoline receptor[1][2]

In Vitro Efaroxan hydrochloride binds to I1-imidazoline and α2-adrenergic receptors in bovine rostral ventrolateral medulla membranes, with Kis of 0.15 and 5.6 nM, respectively[1]
In Vivo Efaroxan hydrochloride increases plasma insulin levels in both conscious fed[3]. Animal Model: Male Sprague-Dawley rats (weight range 250-300g)[3] Dosage: 1 mg/kg, 5 mg/kg Administration: Oral administration Result: Significant increase in plasma insulin levels of starved rats 15 and 30 min after treatment.
References

[1]. T L Berridge, et al. Selectivity profile of the alpha 2-adrenoceptor antagonist efaroxan in relation to plasma glucose and insulin levels in the rat. Eur J Pharmacol. 1992 Mar 24;213(2):205-12.

[2]. A O Abdel-Zaher, et al. The potential antidiabetic activity of some alpha-2 adrenoceptor antagonists. Pharmacol Res. 2001 Nov;44(5):397-409.

[3]. T L Berridge, et al. Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats. Eur J Pharmacol. 1992 Mar 24;213(2):213-8.

 Chemical & Physical Properties

Boiling Point 387ºC at 760 mmHg
Molecular Formula C13H17ClN2O
Molecular Weight 252.740
Flash Point 187.9ºC
Exact Mass 252.102936
PSA 33.62000
LogP 2.33840

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Personal Protective Equipment Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes T: Toxic;
Risk Phrases R25
Safety Phrases 7-35-45
RIDADR UN 2811 6.1/PG 3
HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles31

More Articles
In vivo evaluation of a new ¹⁸F-labeled PET ligand, [¹⁸F]FEBU, for the imaging of I₂-imidazoline receptors.

Nucl. Med. Biol. 42(4) , 406-12, (2015)

The functions of I₂-imidazoline receptors (I₂Rs) are unknown, but evidence exists for their involvement in various neuropsychiatric disorders. Although a few positron emission tomography (PET) I₂R lig...

Repeated exposure to MDMA triggers long-term plasticity of noradrenergic and serotonergic neurons.

Mol. Psychiatry 19(7) , 823-33, (2014)

3,4-Methylenedioxymethamphetamine (MDMA or 'ecstasy') is a psychostimulant drug, widely used recreationally among young people in Europe and North America. Although its neurotoxicity has been extensiv...

Evidence for imidazoline receptors involvement in the agmatine antidepressant-like effect in the forced swimming test.

Eur. J. Pharmacol. 565(1-3) , 125-31, (2007)

This study investigated the involvement of the imidazoline receptors in the antidepressant-like effect of agmatine in the forced swimming test. The antidepressant-like effects of agmatine (10 mg/kg, i...

 Synonyms

Calmidazolium chloride
(±)-efaroxan hydrochloride
2-(2-Ethyl-2,3-dihydro-1-benzofuran-2-yl)-4,5-dihydro-1H-imidazole hydrochloride (1:1)
Efaroxan HCl
1H-Imidazole, 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-, hydrochloride (1:1)
Efaroxan hydrochloride