Drug Information

Drug (ID: DG00795) and It's Reported Resistant Information

• Name: Perphenazine
• Synonyms: Perphenazine; 58-39-9; Trilafon; Perphenazin; Etaperazine; Perfenazine; Ethaperazine; Etaperazin; Fentazin; Chlorpiprazine; Perphenan; Thilatazin; Decentan; Chlorperphenazine; Emesinal; Perfenazina; Tranquisan; Trifaron; Trilifan; Triphenot; F-mon; Perphenazinum; 2-(4-(3-(2-Chloro-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanol; Sch 3940; 2-[4-[3-(2-Chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol; C21H26ClN3OS; 4-[3-(2-Chlorophenothiazin-10-yl)propyl]-1-piperazineethanol; UNII-FTA7XXY4EZ; PZC; gamma-(4-(beta-Hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine; NSC 150866; 4-(3-(2-Chlorophenothiazin-10-yl)propyl)-1-piperazineethanol; 4-[3-(2-Chloro-10H-phenothiazin-10-yl)propyl]-1-piperazineethanol; 1-(2-Hydroxyethyl)-4-(3-(2-chloro-10-phenothiazinyl)propyl)piperazine; 2-{4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl}ethan-1-ol; FTA7XXY4EZ; MFCD00056798; CHEMBL567; 2-Chloro-10-3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl phenothiazine; 2-{4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl}ethanol; 2-Chloro-10-(3-(4-(2-hydroxyethyl)piperazin-1-yl)propyl)phenothiazine; 2-Chloro-10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazine; MLS000069637; CHEBI:8028; 1',1-(2-Idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina; 1-Piperazineethanol, 4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)-; 1-Piperazineethanol, 4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]-; 2-(4-[3-(2-Chloro-10H-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol; NSC150866; NSC-150866; CAS-58-39-9; NCGC00015826-02; Perfenil; SMR000058180; Perfenazina [Italian]; 1-Piperazineethanol, 4-(3-(2-chlorophenothiazin-10-yl)propyl)-; 1-(2-Hydroxyethyl)-4-[3-(2-chloro-10-phenothiazinyl)propyl]piperazine; DSSTox_CID_3441; DSSTox_RID_77031; DSSTox_GSID_23441; Perfenazina [INN-Spanish]; Perphenazinum [INN-Latin]; 1-Piperazineethanol, 4-[3-(2-chlorophenothiazin-10-yl)propyl]-; 2-Chloro-10-3-[1-(2-hydroxyethyl)-4-piperazinyl]propyl phenothiazine; Piperazineethanol, 4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)-; HSDB 3379; SR-01000000137; EINECS 200-381-5; AI3-50151; Piperazineethanol, 4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]-; .gamma.-(4-(.beta.-Hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine; .gamma.-[4-(.beta.-Hydroxyethyl)piperazin-1-yl]propyl-2-chlorophenothiazine; 2-(4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethan-1-ol; Perphenazine [USP:INN:BAN:JAN]; 2-Chloro-10-(3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl)phenothiazine; SCH-3940; Prestwick_536; 1',1-(2-Idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina [Italian]; Etrafon (Salt/Mix); Spectrum_001610; 130-69-8; Opera_ID_1161; Prestwick0_000125; Prestwick1_000125; Prestwick2_000125; Prestwick3_000125; Spectrum2_001602; Spectrum3_000758; Spectrum4_000843; Spectrum5_001493; Lopac-P-6402; P 6402; Lopac0_000930; Oprea1_603835; REGID_for_CID_4748; SCHEMBL42125; BSPBio_000170; BSPBio_002376; GTPL209; KBioGR_001445; KBioSS_002090; MLS001146929; MLS002548897; 5,7-EICOSADIYNOICACID; BIDD:GT0150; DivK1c_000880; SPECTRUM1503934; SPBio_001603; SPBio_002109; BPBio1_000188; DTXSID1023441; component of Triavil (Salt/Mix); HMS502L22; KBio1_000880; KBio2_002090; KBio2_004658; KBio2_007226; KBio3_001596; Perphenazine (JP17/USP/INN); AOB5376; NINDS_000880; HMS1568I12; HMS1922M14; HMS2093M15; HMS2095I12; HMS2232D21; HMS3259C09; HMS3262J22; HMS3370O14; HMS3712I12; HMS3885H20; Pharmakon1600-01503934; HY-A0077; Perphenazine 1.0 mg/ml in Methanol; Tox21_110233; Tox21_500930; 1-Piperazineethanol, trihydrochloride; BDBM50130273; CCG-39060; NSC758649; s4731; STK019818; ZINC19228902; AKOS000664046; Tox21_110233_1; CS-5137; DB00850; KS-5105; LP00930; MCULE-6019566915; NC00472; NSC-758649; SDCCGSBI-0050904.P004; IDI1_000880; MRF-0000509; NCGC00015826-01; NCGC00015826-03; NCGC00015826-04; NCGC00015826-05; NCGC00015826-06; NCGC00015826-07; NCGC00015826-08; NCGC00015826-09; NCGC00015826-10; NCGC00015826-13; NCGC00015826-20; NCGC00024092-03; NCGC00024092-04; NCGC00024092-05; NCGC00024092-06; NCGC00261615-01; AC-12196; SBI-0050904.P003; DB-053200; AB00052390; EU-0072164; EU-0100930; FT-0603244; P1970; C07427; D00503; D82041; J10210; AB00052390_17; A831863; L000919; Q423520; SR-01000000137-2; SR-01000000137-4; SR-01000000137-5; SR-01000000137-8; W-105390; BRD-K10995081-001-05-5; BRD-K10995081-001-15-4; WLN: T C666 BN ISJ EG B3- AT6N DNTJ D2Q; Z1945707494; Perphenazine, British Pharmacopoeia (BP) Reference Standard; Perphenazine, European Pharmacopoeia (EP) Reference Standard; Perphenazine, United States Pharmacopeia (USP) Reference Standard; 2-[4-[3-(2-Chlorophenothiazin-10-yl)propyl]-piperazin-1-yl]ethanol; 2-(4-[3-(2-Chloro-10H-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol #; Perphenazine for system suitability, European Pharmacopoeia (EP) Reference Standard; 2-Chloro-10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazine / 4-[3-(2-Chlorophenothiazin-10-yl)propyl]-1-piperazineethanol
• Indication:
  In total 1 Indication(s)
  Schizophrenia [ICD-11: 6A20]; Approved; [1]
• Target: Dopamine D2 receptor (D2R); DRD2_HUMAN; [1]
• Formula: C21H26ClN3OS
• IsoSMILES: C1CN(CCN1CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO
• InChI: 1S/C21H26ClN3OS/c22-17-6-7-21-19(16-17)25(18-4-1-2-5-20(18)27-21)9-3-8-23-10-12-24(13-11-23)14-15-26/h1-2,4-7,16,26H,3,8-15H2
• InChIKey: RGCVKNLCSQQDEP-UHFFFAOYSA-N
• PubChem CID: 4748
• ChEBI ID: CHEBI:8028
• TTD Drug ID: D02HED
• VARIDT ID: DR00759
• INTEDE ID: DR1264
• DrugBank ID: DB00850

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Brain cancer [ICD-11: 2A00]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Glioblastoma [ICD-11: 2A00.02]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell migration; Inhibition; hsa04670
• Cell Pathway Regulation: Cell invasion; Inhibition; hsa05200
• In Vitro Model: SHI-1 cells; Bone marrow; Homo sapiens (Human); CVCL_2191
• Experiment for Molecule Alteration: Western blotting analysis
• Mechanism Description: The present study explored the effects of perphenazine and prochlorperazine on the levels of ABCB1, ABCG2, E-cadherin, alpha-tubulin and integrins (alpha3, alpha5, and beta1), as well as on the migratory and invasive ability of U87-MG cells. The results suggested that perphenazine and prochlorperazine may modulate the expression levels of multidrug resistance proteins (they decreased ABCB1 and increased ABCG2 expression), E-cadherin, alpha-tubulin and integrins, and could impair the migration and invasion of U-87 MG cells.

Key Molecule: ATP-binding cassette sub-family G2 (ABCG2) [1]

• Molecule Alteration: Expression; Up-regulation
• Sensitive Disease: Glioblastoma [ICD-11: 2A00.02]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell migration; Inhibition; hsa04670
• Cell Pathway Regulation: Cell invasion; Inhibition; hsa05200
• In Vitro Model: SHI-1 cells; Bone marrow; Homo sapiens (Human); CVCL_2191
• Experiment for Molecule Alteration: Western blotting analysis
• Mechanism Description: The present study explored the effects of perphenazine and prochlorperazine on the levels of ABCB1, ABCG2, E-cadherin, alpha-tubulin and integrins (alpha3, alpha5, and beta1), as well as on the migratory and invasive ability of U87-MG cells. The results suggested that perphenazine and prochlorperazine may modulate the expression levels of multidrug resistance proteins (they decreased ABCB1 and increased ABCG2 expression), E-cadherin, alpha-tubulin and integrins, and could impair the migration and invasion of U-87 MG cells.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Integrin alpha-3 (ITA3) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Glioblastoma [ICD-11: 2A00.02]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell migration; Inhibition; hsa04670
• Cell Pathway Regulation: Cell invasion; Inhibition; hsa05200
• In Vitro Model: SHI-1 cells; Bone marrow; Homo sapiens (Human); CVCL_2191
• Experiment for Molecule Alteration: Western blotting analysis
• Mechanism Description: The present study explored the effects of perphenazine and prochlorperazine on the levels of ABCB1, ABCG2, E-cadherin, alpha-tubulin and integrins (alpha3, alpha5, and beta1), as well as on the migratory and invasive ability of U87-MG cells. The results suggested that perphenazine and prochlorperazine may modulate the expression levels of multidrug resistance proteins (they decreased ABCB1 and increased ABCG2 expression), E-cadherin, alpha-tubulin and integrins, and could impair the migration and invasion of U-87 MG cells.

Key Molecule: Integrin beta-1 (ITGB1) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Glioblastoma [ICD-11: 2A00.02]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell migration; Inhibition; hsa04670
• Cell Pathway Regulation: Cell invasion; Inhibition; hsa05200
• In Vitro Model: SHI-1 cells; Bone marrow; Homo sapiens (Human); CVCL_2191
• Experiment for Molecule Alteration: Western blotting analysis
• Mechanism Description: The present study explored the effects of perphenazine and prochlorperazine on the levels of ABCB1, ABCG2, E-cadherin, alpha-tubulin and integrins (alpha3, alpha5, and beta1), as well as on the migratory and invasive ability of U87-MG cells. The results suggested that perphenazine and prochlorperazine may modulate the expression levels of multidrug resistance proteins (they decreased ABCB1 and increased ABCG2 expression), E-cadherin, alpha-tubulin and integrins, and could impair the migration and invasion of U-87 MG cells.

References

• Ref 1: Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, Alpha-tubulin and integrins (Alpha3, Alpha5, and Beta1) levels .Oncol Lett. 2022 Jun;23(6):182. doi: 10.3892/ol.2022.13302. Epub 2022 Apr 15. 10.3892/ol.2022.13302