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Perphenazine
编号 T1090     别名: Perphenazin, Trilafon, Etaperazine
CAS 58-39-9     分子式 C21H26ClN3OS     分子量 403.97
靶点: CAM; Dopamine; 5-HT2Areceptor; Histamine H1 receptor; Alpha-1A adrenergic receptor;
Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
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规格 库存 单价 数量
500 mg 上海现货 479.00
1 g 上海现货 575.00
1 mL * 10 mM (in DMSO) 上海现货 530.00
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生物活性

产品描述

Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

靶点活性

CAM,

Dopamine,

5-HT2Areceptor,

Histamine H1 receptor,

Alpha-1A adrenergic receptor,

体外活性

Perphenazine is a relatively high potency phenothiazine that blocks dopamine 2 (D2) receptors predominantly but also may possess antagonist actions at histamine 1 (H1) and cholinergic M1 and alpha 1 adrenergic receptors in the vomiting center leading to reduced nausea and vomiting[1]. Perphenazine induces cell death and mitochondrial damage, also caspase-3 activation and a decrease in cellular ATP level. The cell death induced by perphenazine is partially suppressed by antioxidant but not by pan-caspase inhibitor[4]. Perphenazine in concentration range from 0.0001 to 0.01 μM did not have any significant effect on melanocytes viability. The treatment of cells with the drug in higher concentrations results in the loss in cell viability in a concentration-dependent manner. The value of EC50 for perphenazine is 2.76 μM. Perphenazine in concentrations of 1.0 and 3.0 μM also decreases the tyrosinase activity, as well as melanin content[5].

体内活性

Perphenazine is well absorbed after oral administration. The time to peak after oral administration is 1-3 hours with the time to peak of the metabolite 7-hydroxyperphenzaine 2-3 hours. Perphenazine has a half-life elimination of 9-12 hours and its metabolite 7-hydroxyperphenazine of 10-19 hours[1]. Perphenazine has been used as a psychotropic drug for several decades in therapy of certain psychiatric disorders. In rat isolated heart, perphenazine significantly prolongs the QT interval and triggers arrhythmias in considerable numbers both at the high concentration and at the therapeutical concentration. This proarrhythmogenic effect is observed even after repeated exposure to perphenazine[3].

细胞实验

cells are plated on 96-well plates and treated with drugs for various time periods. Then the cells are incubated with MTS assay reagent for 1 hr. The plates are then read at 490 nm using a microplate reader.(Only for Reference)

细胞系: human dopaminergic cell line, SH-SY5Y.

动物实验

动物模型:Wistar albino rats

化学信息

分子量

403.97

分子式

C21H26ClN3OS

CAS

58-39-9

溶解度

DMSO: 67 mg/mL (165.9 mM)

Ethanol: 74 mg/mL (183.18 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.475 ml 12.377 ml 24.754 ml
5 mM 0.495 ml 2.475 ml 4.951 ml
10 mM 0.248 ml 1.238 ml 2.475 ml
50 mM 0.05 ml 0.248 ml 0.495 ml
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