您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Perphenazine dihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Perphenazine dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Perphenazine dihydrochloride图片
CAS NO:2015-28-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
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
产品介绍
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)

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%.
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.
Clinical Trial
分子量

476.89

Formula

C21H28Cl3N3OS

CAS 号

2015-28-3

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.