Perphenazine

Catalog No.S4731 Batch:S473101

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Technical Data

Formula

C21H26ClN3OS
Molecular Weight 403.97 CAS No. 58-39-9
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
Targets
D1/D2 dopamine receptors [2]
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].

Protocol (from reference)

Cell Assay:[4]
  • Cell lines

    human dopaminergic cell line, SH-SY5Y.

  • Concentrations

    10-100 μM

  • Incubation Time

    48 h

  • Method

    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.
Animal Study:[2]
  • Animal Models

    Male Wistar albino rats

  • Dosages

    1, 5, and 10 mg/kg

  • Administration

    s.c.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.