Perphenazine

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

奋乃静是典型的抗精神病化合物，抑制5-HT2A受体（5-HT2A）、α-1A肾上腺素受体（α1A）、多巴胺受体D2/D3、D2L受体和组胺H1受体（H1）。

Perphenazine is a typical antipsychotic drug, inhibits 5-HT2A receptor (5-HT2A), Alpha-1A adrenergic receptor (α1A), Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor (H1) with Ki of 5.6, 10, 0.765/0.13, 3.4, and 8 nM.(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.

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.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 Analysis 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 Cell Line:U-87 MG cellsConcentration:1 μMIncubation 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) 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. Animal Model:ICR miceDosage: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 daysResult:Decreased The levels of mice ear swelling.

NSC 150866 | SCH 3940

Endocrinology/Hormones

CaMK

CAM| Dopamine

Neurological Disease

——

58-39-9

403.97

C21H26ClN3OS

>98% (HPLC)

Soluble in DMSO

C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO

2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol

(-20℃)

With Ice Pack

≥ 2 years