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Perphenazine

CAS No. : 58-39-9

MCE 国际站：Perphenazine

产品活性：Perphenazine 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, K_i 值分别为 0.56 nM (D2)、0.43 nM (D3)、0.6 nM (5-HT2A)。Perphenazine 还可与 Alpha-1A 肾上腺素受体 (Alpha-1A adrenergic receptor) 结合。Perphenazine 抑制癌细胞增殖，并诱导细胞凋亡。Perphenazine 可用于精神疾病、癌症、炎症的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation  |  Apoptosis  |  Autophagy

作用靶点：Dopamine Receptor  |  Histamine Receptor  |  5-HT Receptor  |  Adrenergic Receptor  |  Apoptosis  |  Autophagy

In Vitro: Perphenazine (40 μM, 48 h) inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells.
Perphenazine (30 μM, 24 h) 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) inhibits autophagic flux in L02 cells.
Perphenazine (1 µM, 24 h) decreases glioblastoma U-87 MG cell migration and invasion.

In Vivo: Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) induces liver injury and lysosomal membrane damage in ICR mice.
Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis.

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