Formulation: A solid
Formal Name: 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-imidazole, monohydrochloride
Purity: ≥98%
Formula Markup: C13H16N2O • HCl
Formula Weight: 252,7
Shelf life (days): 1460
CAS Number: 89197-00-2
Notes: Efaroxan is an α2-adrenergic receptor (α2-AR; EC50s = 1 receptor antagonist.{52072} It binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 μM.{52073} It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 μM.{52074} Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice.{52075} It also increases 3,4-dihydroxyphenylalanine (L-DOPA; Item No. 13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.{52076}
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