For research use only.
Catalog No.S4731 Synonyms: Perphenazin, Trilafon, Etaperazine
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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|Description||Perphenazine (Perphenazin, Trilafon, Etaperazine) 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. 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. 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.
|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. 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.|
-  Howard S. Smith, et al. Annals od palliative medicine. 2012, 1(2):137-142.
-  Ozdemir E, et al. Bosn J Basic Med Sci. 2013, 13(2):119-25.
-  Kateřina Fialová, et al. Acta Vet. Brno. 2011, 80: 87-92.
|In vitro||DMSO||74 mg/mL (183.18 mM)|
* 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.
|Synonyms||Perphenazin, Trilafon, Etaperazine|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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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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