2015-28-3

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].

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.

D₂ Receptor: 0.56 nM (Ki); D₃ Receptor: 0.43 nM (Ki); D₄ Receptor: 28.5 nM (Ki); 5-HT_2A Receptor: 5.6 nM (Ki); 5-HT₆ Receptor: 17 nM (Ki); 5-HT₇ Receptor: 23 nM (Ki); 5-HT_2C Receptor: 132 nM (Ki); 5-HT_1A Receptor: 421 nM (Ki)

[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