Perphenazine

Perphenazine 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 also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation[1][3][5].

Product Specifications

CAS Number

[58-39-9]

UNSPSC

12352005

Hazard Statement

H302, H317

Target

5-HT Receptor; Adrenergic Receptor; Apoptosis; Autophagy; Dopamine Receptor; Histamine Receptor

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Endocrinology; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Perphenazine.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(Cl)C=C24)CC1

Molecular Formula

C21H26ClN3OS

Molecular Weight

403.97

Precautions

H302, H317

References & Citations

[1]Richtand NM, et al. Dopamine and serotonin receptor binding and antipsychotic efficacy. Neuropsychopharmacology. 2007 Aug;32 (8) :1715-26.|[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. |[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. |[4]Michał Otręba, 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. |[5]Michał Otręba, et al. n vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review. J Appl Toxicol. 2021 Jan;41 (1) :82-94.