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编 号：F748354
分子式：C21H28Cl3N3OS
分子量：476.89
分子式：C21H28Cl3N3OS
分子量：476.89
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CAS No: 2015-28-3
产品详情
生物活性：
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.
体内研究：
Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) dihydrochloride induces liver injury and lysosomal membrane damage in ICR mice.Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) dihydrochloride attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis.Animal Model:ICR mice
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
Dosage:10 mg/kg
Administration:Oral administration, every other day for 6 days
Result:Decreased The levels of mice ear swelling.
体外研究：
Perphenazine (40 μM, 48 h) dihydrochloride inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells.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.Perphenazine (10-40 μM, 24 h) dihydrochloride inhibits autophagic flux in L02 cells.Perphenazine (1 μM, 24 h) dihydrochloride decreases glioblastoma U-87 MG cell migration and invasion.
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.
体内研究：
Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) dihydrochloride induces liver injury and lysosomal membrane damage in ICR mice.Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) dihydrochloride attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis.Animal Model:ICR mice
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
Dosage:10 mg/kg
Administration:Oral administration, every other day for 6 days
Result:Decreased The levels of mice ear swelling.
体外研究：
Perphenazine (40 μM, 48 h) dihydrochloride inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells.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.Perphenazine (10-40 μM, 24 h) dihydrochloride inhibits autophagic flux in L02 cells.Perphenazine (1 μM, 24 h) dihydrochloride decreases glioblastoma U-87 MG cell migration and invasion.
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