Description | (±)-Synephrine is an alkaloid with vasoconstrictor and metabolic activities. It binds to α 1A -, α 2A -, and α 2C -adrenergic receptors (ARs; K i s = 78, 36.7, and 24.4 μM, respectively). (±)-Synephrine is an agonist of α 1A -ARs in HEK293 cells (EC 50 = 4 μM in a reporter assay) but not in CHO cells expressing α 2A - or α 2C -AR. It also acts as an antagonist of α 1A -, α 2A -, and α 2C -ARs, inhibiting L-phenylephrine-induced activation of α 1A -AR in HEK293 cells and activation of α 2A - and α 2C -ARs induced by the α 2 -AR agonist medetomidine in CHO cells (IC 50 s = 12.8, 26, and 27.3 μM, respectively, in reporter assays). (±)-Synephrine induces contractions in isolated rabbit aortic rings (EC 50 = 6.2 μg/ml) and increases ligation-induced mean arterial pressure in rats when administered at a dose of 2 mg/kg per day. It induces lipolysis in isolated rat and human adipocytes when used at concentrations of 100 and 1,000 μg/ml. (±)-Synephrine (50 μM) increases phosphorylation of Akt and AMP-activated protein kinase (AMPK) and translocation of Glut4 to the plasma membrane, as well as increases insulin-induced glucose consumption in L6 muscle cells when used at concentrations ranging from 25 to 200 μM. |
Chemical Properties | Pale Beige Solid |
Uses | A α-adrenergic receptor agonist, vasoconstrictor. |