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Perphenazine

Catalog No. T1090   CAS 58-39-9
Synonyms: Perphenazin, Etaperazine, Trilafon

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

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Perphenazine Chemical Structure
Perphenazine, CAS 58-39-9
Pack Size Availability Price/USD Quantity
50 mg In stock $ 29.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.63%
Purity: 99.36%
Purity: 99.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
Targets&IC50 D2L Receptor:3.4 nM, 5-HT2Areceptor:5.6 nM, Dopamine receptor D2/D3:0.765/0.13 nM, Alpha-1A adrenergic receptor:10 nM, Histamine H1 receptor:8 nM
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].
Cell Research 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)
Synonyms Perphenazin, Etaperazine, Trilafon
Molecular Weight 403.97
Formula C21H26ClN3OS
CAS No. 58-39-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 74 mg/mL (183.18 mM)

DMSO: 67 mg/mL(165.9 mM)

TargetMolReferences and Literature

1. Howard S. Smith, et al. Annals od palliative medicine. 2012, 1(2):137-142. 2. Ozdemir E, et al. Bosn J Basic Med Sci. 2013, 13(2):119-25. 3. Kateřina Fialová, et al. Acta Vet. Brno. 2011, 80: 87-92. 4. Seokheon Hong, et al. Animal Cells and Systems. 2012, 16(1):20-26. 5. Otrba M , Komider L . In vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review[J]. Journal of Applied Toxicology, 2020. 6. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth[J]. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr;8(1): 137-144. 7. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

TargetMolCitations

1. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 2. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr;8(1): 137-144

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library CNS-Penetrant Compound Library Anti-Hypertension Compound Library Drug-induced Liver Injury (DILI) Compound Library ReFRAME Related Library Histamine & Melatonin Receptor-Targeted Compound Library Orally Active Compound Library

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Keywords

Perphenazine 58-39-9 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor Dopamine Receptor 5-HT Receptor CaMK Adrenergic Receptor Autophagy inhibit Serotonin Receptor anti-cancer dermatitis U-87 MG cells Apoptosis Inhibitor lysosome Perphenazin liver injury hepatotoxicity Mental disease Etaperazine Beta Receptor inflammation Trilafon 5-hydroxytryptamine Receptor inhibitor

 

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