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.
For research use only. We do not sell to patients.
- CAS No.: 2015-28-3
- Formula: C21H28Cl3N3OS
- Molecular Weight:476.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Perphenazine dihydrochloride
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Biological Activity
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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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2015-28-3
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Molecular Weight 476.89
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Purity & Documentation
References
[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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