Perphenazine (dihydrochloride)

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]. 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].
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].