Perphenazine dihydrochloride
Based on 3 publication(s) in Google Scholar
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation.
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- CAS No.: 2015-28-3
- Formule: C21H28Cl3N3OS
- Masse moléculaire:476.89
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Perphenazine dihydrochloride
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Activité biologique
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5-HT2A Receptor |
D2 Receptor 0.56 nM (Ki) |
D3 Receptor 0.43 nM (Ki) |
D4 Receptor 28.5 nM (Ki) |
5-HT2A Receptor 5.6 nM (Ki) |
5-HT6 Receptor 17 nM (Ki) |
5-HT7 Receptor 23 nM (Ki) |
5-HT2C Receptor 132 nM (Ki) |
5-HT1A Receptor 421 nM (Ki) |
Perphenazine (40 μM, 48 h) dihydrochloride inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells[2].
Perphenazine (30 μM, 24 h) dihydrochloride induces intense lysosome vacuolation, impaired lysosomal membrane, and induces lysosomal membrane permeabilization (LMP), ultimately triggering lysosomal cell death in L02 cells[2].
Perphenazine (10-40 μM, 24 h) dihydrochloride inhibits autophagic flux in L02 cells[2].
Perphenazine (1 μM, 24 h) dihydrochloride decreases glioblastoma U-87 MG cell migration and invasion[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L02 cells
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Concentration:10-100 μM
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Incubation Time:12, 24, 48 h
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Result:Inhibited cell viability in a concentration and time-dependent manner.
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Cell Line:L02 cells
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Concentration:10, 20, 30, and 40 μM
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Incubation Time:24 h
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Result:Increased LC3 I/II and P62/SQSTM1 levels
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Cell Line:U-87 MG cells
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Concentration:0, 3, 6, 9, 12, and 24 h
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Incubation Time:0, 3, 6, 9, 12, and 24 h
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Result:Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%.
Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) dihydrochloride attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[2]
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Dosage:10, 30, 60, 120, 180 mg/kg
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Administration:Oral gavage, every other day for 21 days.
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Result:Increased histological injury and aminotransferases compared with control.
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Animal Model:Oxazolone-treated animal model of dermatitis[3]
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Dosage:10 mg/kg
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Administration:Oral administration, every other day for 6 days
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Result:Decreased The levels of mice ear swelling.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2015-28-3
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Masse moléculaire 476.89
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Formule C21H28Cl3N3OS
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SMILES
OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(Cl)C=C24)CC1.[H]Cl.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Detachment-Induced FAK-STAT3-NNMT Inhibits CTCs Anoikis to Promote Breast Cancer Metastasis by Enhancing Fatty Acid Oxidation. [Abstract]2026 Mar 12:e22837. PMID: 41816955 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Toxicol Lett
Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo. [Abstract]2022 Aug 15:367:76-87. PMID: 35914675
Pureté et documentation
Références
[1]. Richtand NM, et al. Dopamine and serotonin receptor binding and antipsychotic efficacy. Neuropsychopharmacology. 2007 Aug;32(8):1715-26. [Content Brief]
[2]. Lei Tao, et al. Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo. Toxicol Lett. 2022 Jul 29;367:76-87. [Content Brief]
[3]. Min-Jeong Heo, et al. Perphenazine Attenuates the Pro-Inflammatory Responses in Mouse Models of Th2-Type Allergic Dermatitis. Int J Mol Sci. 2020 May 3;21(9):3241. [Content Brief]
[4]. Michał Otręba, et al. Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, α-tubulin and integrins (α3, α5, and β1) levels. Oncol Lett. 2022 Jun;23(6):182. [Content Brief]
[5]. Michał Otręba, et al. n vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review. J Appl Toxicol. 2021 Jan;41(1):82-94. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Perphenazine dihydrochloride Related Classifications
HY-A0077A Related Classifications
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