CAS 89197-00-2|Efaroxan hydrochloride
| Common Name | Efaroxan hydrochloride | ||
|---|---|---|---|
| CAS Number | 89197-00-2 | Molecular Weight | 252.740 |
| Density | / | Boiling Point | 387ºC at 760 mmHg |
| Molecular Formula | C13H17ClN2O | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 187.9ºC |
| Symbol | GHS06 | Signal Word | Danger |
Names
| Name | 2-(2-ethyl-3H-1-benzofuran-2-yl)-4,5-dihydro-1H-imidazole,hydrochloride |
|---|---|
| Synonym | More Synonyms |
Efaroxan hydrochloride BiologicalActivity
| 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 ReceptorResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>GPCR/G Protein >>Imidazoline ReceptorSignaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorResearch 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 |
| InChIKey | DWOIUCRHVWIHAH-UHFFFAOYSA-N |
| SMILES | CCC1(C2=NCCN2)Cc2ccccc2O1.Cl |
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% |
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 |
