Perphenazine

製品コードS4731 バッチS473101

印刷

化学情報

Chemical Structure Synonyms Perphenazin, Trilafon, Etaperazine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H26ClN3OS
分子量 403.97 CAS No. 58-39-9
Solubility (25°C)* 体外 DMSO 74 mg/mL (183.18 mM)
Ethanol 74 mg/mL (183.18 mM)
Water Insoluble
* <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 Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
in vitro Perphenazine is a relatively high potency phenothiazine that blocks dopamine 2 (D2) receptors predominantly but also may possess antagonist actions at histamine 1 (H1) and cholinergic M1 and alpha 1 adrenergic receptors in the vomiting center leading to reduced nausea and vomiting[1]. Perphenazine induces cell death and mitochondrial damage, also caspase-3 activation and a decrease in cellular ATP level. The cell death induced by perphenazine is partially suppressed by antioxidant but not by pan-caspase inhibitor[4]. Perphenazine in concentration range from 0.0001 to 0.01 µM did not have any significant effect on melanocytes viability. The treatment of cells with the drug in higher concentrations results in the loss in cell viability in a concentration-dependent manner. The value of EC50 for perphenazine is 2.76 μM. Perphenazine in concentrations of 1.0 and 3.0 µM also decreases the tyrosinase activity, as well as melanin content[5].
in vivo Perphenazine is well absorbed after oral administration. The time to peak after oral administration is 1-3 hours with the time to peak of the metabolite 7-hydroxyperphenzaine 2-3 hours. Perphenazine has a half-life elimination of 9-12 hours and its metabolite 7-hydroxyperphenazine of 10-19 hours[1]. Perphenazine has been used as a psychotropic drug for several decades in therapy of certain psychiatric disorders. In rat isolated heart, perphenazine significantly prolongs the QT interval and triggers arrhythmias in considerable numbers both at the high concentration and at the therapeutical concentration. This proarrhythmogenic effect is observed even after repeated exposure to perphenazine[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human dopaminergic cell line, SH-SY5Y.
濃度 10-100 μM
反応時間 48 h
実験の流れ cells are plated on 96-well plates and treated with drugs for various time periods. Then the cells are incubated with MTS assay reagent for 1 hr. The plates are then read at 490 nm using a microplate reader.
動物実験 動物モデル Male Wistar albino rats
投薬量 1, 5, and 10 mg/kg
投与方法 s.c.

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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