Perphenazine
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.
| 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 |
| SDF | Download SDF |
| Canonical SMILES | OCCN1CCN(CCCN2c(cc(cc3)Cl)c3Sc3c2cccc3)CC1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[3] | |
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Cell lines |
Human dopaminergic neuroblastoma SH-SY5Y cells |
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Reaction Conditions |
10 ~ 100 μM perphenazine for 48 h incubation |
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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] | |
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Animal models |
Male Wistar albino rats, 190-205 g |
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Dosage form |
1, 5 and 10 mg/kg Subcutaneous injection |
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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. |
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Note |
The technical data provided above is for reference only. |
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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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