Perphenazine

For research use only.

Catalog No.S4731 Synonyms: Perphenazin, Trilafon, Etaperazine

Perphenazine Chemical Structure

CAS No. 58-39-9

Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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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

Cell Research:[4]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Male Wistar albino rats
  • Dosages: 1, 5, and 10 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (183.18 mM)
Water Insoluble
Ethanol ''74 mg/mL

* 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.

Chemical Information

Molecular Weight 403.97
Formula

C21H26ClN3OS

CAS No. 58-39-9
Storage powder
in solvent
Synonyms Perphenazin, Trilafon, Etaperazine
Smiles C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00737256 Unknown status Drug: Aripiprazole|Drug: Perphenazine Schizophrenia|Cocaine Dependence Paul Saenger|Denver Research Institute August 2008 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID