Perphenazine dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Perphenazine dihydrochloride 是一种具有口服活性的多巴胺受体 (dopamine receptor) 和组胺-1 受体 (histamine-1 receptor) 拮抗剂, Ki 值分别为 0.56 nM (D2)、0.43 nM (D3)、0.6 nM (5-HT2A)。Perphenazine dihydrochloride 还可与 Alpha-1A 肾上腺素受体 (Alpha-1A adrenergic receptor) 结合。Perphenazine dihydrochloride 抑制癌细胞增殖，并诱导细胞凋亡 (apoptosis)。Perphenazine dihydrochloride 可用于精神疾病、癌症、炎症的研究。

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.

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.Cell Viability Assay 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 AnalysisCell Line:L02 cells Concentration:10, 20, 30, and 40 μM Incubation Time:24 h Result:Increased LC3 I/II and P62/SQSTM1 levelsCell Migration Assay 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%.

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.

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GPCR/G Protein

Dopamine Receptor

Dopamine Receptor | 5-HT Receptor | Apoptosis | Histamine Receptor

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2015-28-3

476.89

C21H28Cl3N3OS

>98% (HPLC)

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ClC1=CC=C2SC3=C(N(CCCN4CCN(CC4)CCO)C2=C1)C=CC=C3.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years