Perphenazine

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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。

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 Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	403.97
Cas No.	58-39-9
Formula	C₂₁H₂₆ClN₃OS
Solubility	insoluble in H2O; ≥104.6 mg/mL in EtOH; ≥111.6 mg/mL in DMSO
Chemical Name	2-(4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanol
Canonical SMILES	ClC1=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, α_1A-, α_2A-, α_2B-, and α_2C-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.