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Prochlorperazine

 
Catalog No.
A8508
多巴胺(D2)受体拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 545.00
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100mg
¥ 190.00
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1g
¥ 227.00
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A

背景

Prochlorperazine (Compazine, Stemzine, Buccastem, Stemetil, Phenotil) is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly potent typical antipsychotic, 10-20x more potent than chlorpromazine. It is also used to treat migraine headaches. Intravenous administration can be used to treat status migrainosus.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt373.94
Cas No.58-38-8
FormulaC20H24ClN3S
Solubilityinsoluble in H2O; ≥16.5 mg/mL in DMSO; ≥58.5 mg/mL in EtOH
Chemical Name2-chloro-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine
SDFDownload SDF
Canonical SMILESCN(CC1)CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(Cl)C=C4
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试验操作

Cell experiment:[1]

Cell lines

BT474 cells

Reaction Conditions

5 μM prochlorperazine for 2 or 5 d incubation

Applications

In BT474 cells that over-express HER2 and have previously been shown to be tamoxifen resistant, treatment with 5 μM of prochlorperazine in the presence or absence of 4-hydroxytamoxifen significantly inhibited cell proliferation and reduced cyclin E2 mRNA levels. Prochlorperazine has the potential to inhibit proliferation of tamoxifen-resistant breast tumors.

Animal experiment:[2]

Animal models

Beagle dogs, 8 ~ 16 kg

Dosage form

0.34 mg/kg

Administered subcutaneously

Applications

Prochlorperazine inhibited emesis induced by apomorphine in dogs, with an ED50 value of 0.34 mg/kg.

Note

The technical data provided above is for reference only.

References:

1. Huang L, Zhao S, Frasor JM, et al. An integrated bioinformatics approach identifies elevated cyclin E2 expression and E2F activity as distinct features of tamoxifen resistant breast tumors. PLoS One, 2011, 6(7): e22274.

2. Niemegeers CJ. Antiemetic specificity of dopamine antagonists. Psychopharmacology (Berl), 1982, 78(3): 210-213.

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