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Perphenazine
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图片
CAS NO:58-39-9
包装与价格:
包装价格(元)
1g电议
5g电议

产品介绍

化学性质

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
Canonical SMILESClC1=CC(N(C2=CC=CC=C2S3)CCCN4CCN(CCO)CC4)=C3C=C1
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

Perphenazine blocks dopamine D2receptors 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 H1receptors, withKivalues 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.

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 D2receptors. 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.