Perphenazine 是吩噻嗪衍生物和多巴胺拮抗剂，具有止吐和抗精神病特性。它能够抑制5-HT2A受体，α1A肾上腺素能受体，多巴胺D2、D3、D2L受体，以及组胺H1受体，对应的Ki值分别为5.6、10、0.765、0.13、3.4 和 8 nM。

Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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].

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].

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.(Only for Reference)

58-39-9

C21H26ClN3OS

403.97

Etaperazine;奋乃静;Perphenazin;Trilafon

Ethanol:74 mg/mL (183.18 mM)
DMSO:67 mg/mL(165.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years