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Apoptosis" style="display: inline; color: #c13a36">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 K i 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].

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]. 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%.

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]. 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.

2015-28-3

C21H28Cl3N3OS

476.89

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years