Home Neuronal Signaling Dopamine Receptor antagonist Perphenazine For research use only.

Perphenazine

Synonyms: Perphenazin, Trilafon, Etaperazine

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

Perphenazine Chemical Structure

Perphenazine Chemical Structure

CAS: 58-39-9

Purity & Quality Control

Batch: S473101 DMSO] 74 mg/mL] false] Ethanol] 74 mg/mL] false] Water] Insoluble] false Purity: 99.89%
99.89

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Male Wistar albino rats
Dosages 1, 5, and 10 mg/kg
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00737256 Unknown status Schizophrenia|Cocaine Dependence Paul Saenger|Denver Research Institute August 2008 Phase 2

Chemical lnformation & Solubility

Molecular Weight 403.97 Formula

C21H26ClN3OS
CAS No. 58-39-9 SDF Download Perphenazine SDF
Smiles C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (183.18 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 74 mg/mL

Water : Insoluble


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In vivo
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