| Identification | Back Directory | [Name]
4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride | [CAS]
2015-28-3 | [Synonyms]
PERPHENAZINE HCL
Perphenazine hydrochloride
4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride | [EINECS(EC#)]
217-944-6 | [Molecular Formula]
C21H28Cl3N3OS | [MOL File]
2015-28-3.mol | [Molecular Weight]
476.891 |
| Hazard Information | Back Directory | [Uses]
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation[1][3][5]. | [Safety Profile]
Poison by ingestion, intraperitoneal, intravenous, and intramuscular routes. Moderately toxic by subcutaneous route. When heated to decomposition it emits very toxic fumes of Clí, NOx, SOx, and HCl. | [in vivo]
Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) dihydrochloride induces liver injury and lysosomal membrane damage in ICR mice[2].
Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) dihydrochloride attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis[3]. | Animal Model: | ICR mice[2] | | Dosage: | 10, 30, 60, 120, 180 mg/kg | | Administration: | Oral gavage, every other day for 21 days. | | Result: | Increased histological injury and aminotransferases compared with control. |
| Animal Model: | Oxazolone-treated animal model of dermatitis[3] | | Dosage: | 10 mg/kg | | Administration: | Oral administration, every other day for 6 days | | Result: | Decreased The levels of mice ear swelling. |
| [IC 50]
D2 Receptor: 0.56 nM (Ki); D3 Receptor: 0.43 nM (Ki); D4 Receptor: 28.5 nM (Ki); 5-HT2A Receptor: 5.6 nM (Ki); 5-HT6 Receptor: 17 nM (Ki); 5-HT7 Receptor: 23 nM (Ki); 5-HT2C Receptor: 132 nM (Ki); 5-HT1A Receptor: 421 nM (Ki) | [References]
[1] Richtand NM, et al. Dopamine and serotonin receptor binding and antipsychotic efficacy. Neuropsychopharmacology. 2007 Aug;32(8):1715-26. DOI:10.1038/sj.npp.1301305
[2] Lei Tao, et al. Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo. Toxicol Lett. 2022 Jul 29;367:76-87. DOI:10.1016/j.toxlet.2022.07.814
[3] Min-Jeong Heo, et al. Perphenazine Attenuates the Pro-Inflammatory Responses in Mouse Models of Th2-Type Allergic Dermatitis. Int J Mol Sci. 2020 May 3;21(9):3241. DOI:10.3390/ijms21093241
[4] Micha? Otr?ba, et al. Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, α-tubulin and integrins (α3, α5, and β1) levels. Oncol Lett. 2022 Jun;23(6):182. DOI:10.3892/ol.2022.13302
[5] Micha? Otr?ba, et al. n vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review. J Appl Toxicol. 2021 Jan;41(1):82-94. DOI:10.1002/jat.4046 |
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