Perphenazine

SKU: orb1309806

Description

Perphenazine

Research Area

Neuroscience

Key Properties

• CAS Number: 58-39-9
• MW: 403.98
• Purity: >98%
• Formula: C₂₁H₂₆ClN₃OS
• SMILES: OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(Cl)C=C3)CC1
• Target: Monoamine receptor
• Solubility: Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 5 mg/ml)

Bioactivity

• Target IC50:
  H2 receptor:132 nM (Ki)|D2L receptor:3.4 nM|D2 Receptor:0.765 nM|D2 Receptor:0.56 nM (Ki)|5-HT6 receptor:17 nM (Ki)|5-HT1A receptor:421 nM (Ki)|5-HT7 receptor:23 nM (Ki)|D4 Receptor:28.5 nM (Ki)|5-HT2A receptor:5.6 nM|D3 receptor:0.13 nM|D3 receptor:0.43 nM (Ki)|α1A-adrenoceptor:10 nM|H1 receptor:8 nM
• 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.
• 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. 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.
• 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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Trilafon, Perphenazin, Perphenazine, Serotonin Receptor, U-87 MG cells, α1A-adrenergic receptor, Inhibitor, HistamineReceptor, Histamine Receptor, hepatotoxicity, Mental disease, H1 receptor, Etaperazine, inflammation, inhibit, liver injury, lysosome, 5HTReceptor, 5-hydroxytryptamine Receptor, 5HT Receptor, AdrenergicReceptor, Adrenergic Receptor, 5-HT Receptor, 5-HT2A, CAM, anti-cancer, Apoptosis, Autophagy, Beta Receptor, Dopamine Receptor, Dopamine, DopamineReceptor, dermatitis

Compound Identifiers

PubChem CID

4748