Synephrine HCl

製品コードS2438 バッチS243801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H13NO2.HCl
分子量 203.67 CAS No. 5985-28-4
Solubility (25°C)* 体外 Water 41 mg/mL (201.3 mM)
DMSO 14 mg/mL (68.73 mM)
Ethanol 4 mg/mL (19.63 mM)
体内 （毎回新しく調製した物を用意してください）
Clear solution
Saline
30.0mg/ml Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 SynephrineHCl (Oxedrine, p-Synephrine) is a sympathomimetic α-adrenergic receptor (AR) agonist.
in vitro Synephrine (0.1-30 μM) displays potent vasoconstrictive effects on isolated rat aorta in a dose dependent manner, which can be significantly inhibited by pretreatment with prazosin, BRL15572, and ketanserin but not by pretreatment with SB216641 and propranolol, indicating that Synephrine exerts the constrictive effects via adrenergic alpha(1)-receptors, serotonergic 5-HT(1D) receptors, and 5-HT(2A) receptors. [2] Although the Ki values of Synephrine, 1R,2S-norephedrine, and β-phenethylamine are same for all three subtypes, only Synephrine is a partial agonist of α1A-AR subtype stably expressed in HEK 293 cells with EC50 of 4 µM, giving a maximal response at 100 µM that is equal to 55.3 % of the L-phenylephrine maximum. Functional studies on the α2A- and α2C-AR subtypes stably expressed in CHO cells indicate that Synephrine may act as an antagonist rather than an agonist of the pre-synaptic α(2A)- and α(2C)-AR subtypes present in nerve terminals, although antagonist activity of synephrine is lower than its partial agonist potency. [3] Synephrine (~100 μM) treatment increases basal glucose consumption up to 50% over the control in a dose-dependent manner, without affecting the viability of L6 skeletal muscle cells. Synephrine significantly stimulates the basal- or insulin-stimulated lactic acid production as well as glucose consumption. Synephrine treatment stimulates the phosphorylation of AMPK but not Akt, and Synephrine-induced glucose consumption and the translocation of Glut4 from the cytoplasm to the plasma membrane are sensitive to the inhibition of AMPK but not to the inhibition of PI3 kinase. [4]
in vivo Administration of Synephrine (1 mg/kg per 12 hours) for 8 days significantly improves the hyperdynamic state in portal hypertensive rats induced by either partial portal vein ligation (PVL) or bile duct ligation (BDL), and significantly reduces the portal venous pressure, portal tributary blood flow and cardiac index in both PVL and BDL rats. [1]

プロトコル(参考用のみ)

動物実験 動物モデル Male Sprague-Dawley rats with portal hypertension (with or without cirrhosis) induced by bile duct ligation or partial portal vein ligation
投薬量 ~1 mg/kg per 12 hours
投与方法 Oral gavage

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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