Efaroxan hydrochloride

Names

[ Name ]:
Efaroxan hydrochloride

[Synonym ]:
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

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]:

Signaling Pathways >> Neuronal Signaling >> Imidazoline Receptor

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Imidazoline Receptor

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Metabolic Disease

[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

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

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%

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...