CAS NO: | 58-39-9 |
包装 | 价格(元) |
1g | 电议 |
5g | 电议 |
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。 |
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.
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. |