Efaroxan hydrochloride manufacturers
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| | Efaroxan hydrochloride Basic information |
| Product Name: | Efaroxan hydrochloride | | Synonyms: | 2-ETHYL-2-(IMIDAZOLIN-2-YL)-2,3-DIHYDROBENZOFURAN HYDROCHLORIDE;(+/-)-2-(2-ETHYL-2,3-DIHYDRO-2-BENZOFURANYL)-4,5-DIHYDRO-1H-IMIDAZOLE HYDROCHLORIDE;2-(2-Ethyl-2,3-dihydrobenzofuran-2-yl)-4,5-dihydro-1H-imidazole hydrochloride;EfaroxanHCl;RX 821037A, 2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran hydrochloride;Zinc00002748;RX 821037A;1H-Imidazole,2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-,monohydrochloride | | CAS: | 89197-00-2 | | MF: | C13H17ClN2O | | MW: | 252.74 | | EINECS: | | | Product Categories: | Adrenoceptor | | Mol File: | 89197-00-2.mol |  |
| | Efaroxan hydrochloride 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 |
| 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 |
| | Efaroxan hydrochloride 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 |
| | Efaroxan hydrochloride Preparation Products And Raw materials |
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