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Perphenazine

奋乃静
Catalog No.
B6157
多巴胺拮抗剂
组合的产品项目
规格价格库存 数量
1g
¥ 545.00
现货
5g
¥ 1,090.00
现货

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A

背景

Perphenazine blocks dopamine D2 receptors predominantly, but also may possess antagonist actions against histamine H1, cholinergic M1 and α1-adrenergic receptors in the vomiting center leading to reduced nausea and vomiting. Perphenazine binds to dopamine D2, α1A-, α2A-, α2B-, and α2C-adrenergic, M3 muscarinic, and histamine H1 receptors, with Ki values being 1.4, 10, 810.5, 104.9, 85.2, 1848 and 8 nM, respectively. Formulations containing perphenazine have been used for the treatment of schizophrenia and psychosis. The potency of its antiemetic effects is intermediate.

References:

1. Smith HS, Cox LR, Smith BR. Dopamine receptor antagonists. Annals of Palliative Medicine, 2012, 1(2): 137-142.

2. Kroeze WK, Hufeisen SJ, Popadak BA, et al. H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology, 2003, 28(3): 519-526.

3. Hong S, Lee M, Shin KS, et al. Perphenazine and trifluoperazine induce mitochondria-mediated cell death in SH-SY5Y cells, Animal Cells and Systems, 2012, 16(1): 20-26.

4. Ozdemir E, Bagcivan I, Gursoy S. Role of D₁/D₂ dopamin receptors antagonist perphenazine in morphine analgesia and tolerance in rats. Bosnian Journal of Basic Medical Sciences, 2013, 13(2): 119-125.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt403.97
Cas No.58-39-9
FormulaC21H26ClN3OS
Solubilityinsoluble in H2O; ≥104.6 mg/mL in EtOH; ≥111.6 mg/mL in DMSO
Chemical Name2-(4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanol
SDFDownload SDF
Canonical SMILESClC1=CC(N(C2=CC=CC=C2S3)CCCN4CCN(CCO)CC4)=C3C=C1
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试验操作

Cell experiment:[3]

Cell lines

Human dopaminergic neuroblastoma SH-SY5Y cells

Reaction Conditions

10 ~ 100 μM perphenazine for 48 h incubation

Applications

SH-SY5Y cells treated with perphenazine at 25 µM showed fragmented mitochondria as early as 4 hr after the drug treatment when the cell death was not evident. At 48 hr, perphenazine induced about 80% cell death at a concentration of 25 µM.

Animal experiment:[4]

Animal models

Male Wistar albino rats, 190-205 g

Dosage form

1, 5 and 10 mg/kg

Subcutaneous injection

Applications

Perphenazine was capable of suppressing opioid tolerance, possibly by the mechanism of inhibiting dopamine D2 receptors. The maximum analgesic effect was observed at 60 min after administration of 10 mg/kg perphenazine.

Note

The technical data provided above is for reference only.

References:

1. Smith HS, Cox LR, Smith BR. Dopamine receptor antagonists. Annals of Palliative Medicine, 2012, 1(2): 137-142.

2. Kroeze WK, Hufeisen SJ, Popadak BA, et al. H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology, 2003, 28(3): 519-526.

3. Hong S, Lee M, Shin KS, et al. Perphenazine and trifluoperazine induce mitochondria-mediated cell death in SH-SY5Y cells, Animal Cells and Systems, 2012, 16(1): 20-26.

4. Ozdemir E, Bagcivan I, Gursoy S. Role of D₁/D₂ dopamin receptors antagonist perphenazine in morphine analgesia and tolerance in rats. Bosnian Journal of Basic Medical Sciences, 2013, 13(2): 119-125.

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