2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis Autophagy
  3. Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy
  4. Perphenazine dihydrochloride

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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Perphenazine dihydrochloride Chemical Structure

Perphenazine dihydrochloride Chemical Structure

CAS No. : 2015-28-3

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Perphenazine dihydrochloride Related Antibodies

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1 Publications Citing Use of MCE Perphenazine dihydrochloride

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Description

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[1][3][5].

IC50 & Target[1]

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)

In Vitro

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.

Perphenazine dihydrochloride Related Antibodies

Cell Viability Assay[2]

Cell Line: L02 cells
Concentration: 10-100 μM
Incubation Time: 12, 24, 48 h
Result: Inhibited cell viability in a concentration and time-dependent manner.

Western Blot Analysis[2]

Cell Line: L02 cells
Concentration: 10, 20, 30, and 40 μM
Incubation Time: 24 h
Result: Increased LC3 I/II and P62/SQSTM1 levels

Cell Migration Assay [4]

Cell Line: U-87 MG cells
Concentration: 0, 3, 6, 9, 12, and 24 h
Incubation Time: 0, 3, 6, 9, 12, and 24 h
Result: Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%.
In Vivo

Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) dihydrochloride induces liver injury and lysosomal membrane damage in ICR mice[2].
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.

Animal Model: ICR mice[2]
Dosage: 10, 30, 60, 120, 180 mg/kg
Administration: Oral gavage, every other day for 21 days.
Result: Increased histological injury and aminotransferases compared with control.
Animal Model: Oxazolone-treated animal model of dermatitis[3]
Dosage: 10 mg/kg
Administration: Oral administration, every other day for 6 days
Result: Decreased The levels of mice ear swelling.
Clinical Trial
Molecular Weight

476.89

Formula

C21H28Cl3N3OS
CAS No.
SMILES

OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(Cl)C=C24)CC1.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Perphenazine dihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Perphenazine2015-28-3Dopamine ReceptorHistamine Receptor5-HT ReceptorAdrenergic ReceptorApoptosisAutophagySerotonin Receptor5-hydroxytryptamine ReceptorBeta ReceptorMental diseaseliver injuryhepatotoxicitydermatitisinflammationU-87 MG cellsanti-cancerlysosomeInhibitorinhibitorinhibit

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