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。
| 生物活性 | Perphenazine dihydrochloride is an orally activedopamine receptorandhistamine-1 receptorantagonist, withKivalues of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds toAlpha-1Aadrenergic receptor. Perphenazine dihydrochloride inhibitscancercell proliferation, and inducesapoptosis. Perphenazine dihydrochloride can be used in the research of mental disease,cancer, inflammation[1][3][5]. |
| IC50& Target[1] | D2Receptor 0.56 nM (Ki) | D3Receptor 0.43 nM (Ki) | D4Receptor 28.5 nM (Ki) | 5-HT2AReceptor 5.6 nM (Ki) | 5-HT6Receptor 17 nM (Ki) | 5-HT7Receptor 23 nM (Ki) | 5-HT2CReceptor 132 nM (Ki) | 5-HT1AReceptor 421 nM (Ki) |
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体外研究
(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].
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%. |
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体内研究
(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].
| 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. |
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| Clinical Trial | |
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| 中文名称 | 奋乃静二盐酸盐；过非那嗪二盐酸盐；羟哌氯丙嗪二盐酸盐；丕芬那辛二盐酸盐 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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