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説明

(±)-Synephrine is an alkaloid with vasoconstrictor and metabolic activities. It binds to α_1A-, α_2A-, and α_2C-adrenergic receptors (ARs; K_is = 78, 36.7, and 24.4 μM, respectively). (±)-Synephrine is an agonist of α_1A-ARs in HEK293 cells (EC₅₀ = 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 α₂-AR agonist medetomidine in CHO cells (IC₅₀s = 12.8, 26, and 27.3 μM, respectively, in reporter assays). (±)-Synephrine induces contractions in isolated rabbit aortic rings (EC₅₀ = 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.