product name Perphenazine
Description: Perphenazine (also known as Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. Perphenazine has relatively high potency and 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.
References: Bosn J Basic Med Sci. 2013 May;13(2):119-25; Biochem Pharmacol. 1990 Apr 1;39(7):1167-73.
403.97
Formula
C21H26ClN3OS
CAS No.
58-39-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (183.2 mM)
Water: <1 mg/mL
Ethanol: 74 mg/mL (183.2 mM)
Solubility (In vivo)
Synonyms
Perphenazine, Perphenazin, Trilafon, Etaperazine
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19414744
| In Vitro |
In vitro activity: 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. Kinase Assay: Perphenazine is a typical antipsychotic drug, inhibits 5-HT2A receptor (5-HT2A), Alpha-1A adrenergic receptor (α1A), Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor (H1) with Ki of 5.6, 10, 0.765/0.13, 3.4, and 8 nM. IC50 value: 5.6 nM (Ki, 5-HT2A) 10 nM (Ki,α1A), 0.765/0.13 nM (Ki,D2/D3), 3.4 nM (Ki,D2L receptor), 8 nM (Ki,H1). Cell Assay: 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 | 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. |
| Animal model | Male Wistar albino rats |
| Formulation & Dosage | Dissolved in saline; 1, 5, and 10 mg/kg; s.c. |
| References | Bosn J Basic Med Sci. 2013 May;13(2):119-25; Acta Vet. Brno. 2011, 80: 87-92; Biochem Pharmacol. 1990 Apr 1;39(7):1167-73. |
