4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride

Modify Date: 2025-08-26 20:51:25

4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride structure	Common Name	4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride
	CAS Number	2015-28-3	Molecular Weight	476.89100
	Density	N/A	Boiling Point	580.4ºC at 760mmHg
	Molecular Formula	C₂₁H₂₈Cl₃N₃OS	Melting Point	N/A
	MSDS	N/A	Flash Point	304.8ºC

Use of 4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride

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].

Name	2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol,dihydrochloride
Synonym	More Synonyms

Description	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].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
Target	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)
In Vitro	Perphenazine dihydrochloride (40 μM, 48 h) inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells[2]. Perphenazine dihydrochloride (30 μM, 24 h) induces intense lysosome vacuolation, impaired lysosomal membrane, and induces lysosomal membrane permeabilization (LMP), ultimately triggering lysosomal cell death in L02 cells[2]. Perphenazine dihydrochloride (10-40 μM, 24 h) inhibits autophagic flux in L02 cells[2]. Perphenazine dihydrochloride (1 µM, 24 h) decreases glioblastoma U-87 MG cell migration and invasion[4]. Cell Viability Assay[2] Cell Line: L02 cells Concentration: 10-100 μM Incubation Time: 12, 24, 48 h Result: Inhibited cell viability in a concentration and time-dependent manner. Western Blot Analysis[2] Cell Line: L02 cells Concentration: 10, 20, 30, and 40 μM Incubation Time: 24 h Result: Increased LC3 I/II and P62/SQSTM1 levels Cell Migration Assay [4] Cell Line: U-87 MG cells Concentration: 0, 3, 6, 9, 12, and 24 h Incubation Time: 0, 3, 6, 9, 12, and 24 h Result: Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%.
In Vivo	Perphenazine dihydrochloride (oral gavage, 180 mg/kg, every other day for 21 days) induces liver injury and lysosomal membrane damage in ICR mice[2]. Perphenazine dihydrochloride (oral administration, 10 mg/kg, every other day for 6 days) 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.
References	[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.

Boiling Point	580.4ºC at 760mmHg
Molecular Formula	C₂₁H₂₈Cl₃N₃OS
Molecular Weight	476.89100
Flash Point	304.8ºC
Exact Mass	475.10200
PSA	55.25000
LogP	5.48750
Vapour Pressure	2.6E-14mmHg at 25°C
Storage condition	2-8°C

Perphenazin-dihydrochlorid

EINECS 217-944-6

Perphenazine HCl

Perphenazine dihydrochloride

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4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride

Use of 4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazine-1-ethanol dihydrochloride

Names

Biological Activity

Chemical & Physical Properties

Synonyms

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.