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Perphenazine Dopamine Receptor antagonist

Cat.No.S4731

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

Chemical Structure

Molecular Weight: 403.97

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (183.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 74 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 403.97 Formula

C21H26ClN3OS

 Storage (From the date of receipt)
CAS No. 58-39-9 Download SDF Storage of Stock Solutions

Synonyms Perphenazin, Trilafon, Etaperazine Smiles C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO

Mechanism of Action

Targets/IC50/Ki
D1/D2 dopamine receptors
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. This compound induces cell death and mitochondrial damage, also caspase-3 activation and a decrease in cellular ATP level. The cell death induced by this chemical is partially suppressed by antioxidant but not by pan-caspase inhibitor. This drug 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 this compound is 2.76 μM. It in concentrations of 1.0 and 3.0 µM also decreases the tyrosinase activity, as well as melanin content.
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. This compound has a half-life elimination of 9-12 hours and its metabolite 7-hydroxyperphenazine of 10-19 hours. It has been used as a psychotropic drug for several decades in therapy of certain psychiatric disorders. In rat isolated heart, this chemical 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 this compound.
References
  • [4] http://china.tandfonline.com/doi/abs/10.1080/19768354.2011.611256
  • [5] http://www.ptfarm.pl/pub/File/Acta_Poloniae/2016/nr%204/903.pdf

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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