General Information of Drug (ID: DM0DJ9O)

Drug Name
Flupentixol Drug Info
Synonyms
2-[4-[(3Z)-3-[2-(Trifluoromethyl)thioxanthen-9-ylidene]propyl]piperazin-1-yl]ethanol; 4-(3-(2-(Trifluoromethyl)thioxanthen-9-ylidene)propyl)-1-piperazineethanol; 53772-82-0; ALPHA-FLUPENTHIXOL; EINECS 220-304-9; EINECS 258-756-4; Emergil; FA0UYH6QUO; FLUPENTHIXOL; Fluanxol; Flupenthixole; Flupentixol; Flupentixolum [INN-Latin]; Fluphenthixol; Fluxanxol; LC 44; N 7009; Siplaril; Siplarol; UNII-FA0UYH6QUO; cis-(Z)-Flupenthixol; cis-(Z)-Flupenthixol dihydrochloride; cis-Flupenthixol; cis-Flupentixol; flupentixolum
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Approved [1]
Therapeutic Class
Antipsychotic Neuroleptic drug
Cross-matching ID
PubChem CID
5281881
ChEBI ID
CHEMBL54661
CAS Number
CAS 2709-56-0
TTD Drug ID
DM0DJ9O
VARIDT Drug ID
DR01298

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [5]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [6]
Methotrexate DM2TEOL Anterior urethra cancer Approved [7]
Folic Acid DMEMBJC Colorectal carcinoma Approved [8]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [7]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [7]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [9]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [7]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [10]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [12]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [13]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [14]
Cepharanthine DM9Y5JB N. A. N. A. Approved [15]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [16]
Clozapine DMFC71L Schizophrenia 6A20 Approved [17]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [18]
Trifluoperazine DMKBYWI Anxiety Approved [19]
Olanzapine DMPFN6Y Bipolar depression Approved [17]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [14]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By D(1A) dopamine receptor (DRD1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [20]
Haloperidol DM96SE0 Delirium Approved [21]
Pergolide mesylate DM5GKOV N. A. N. A. Approved [22]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [21]
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [23]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [24]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [25]
Methamphetamine DMPM4SK Anxiety Approved [26]
Clozapine DMFC71L Schizophrenia 6A20 Approved [27]
Bardoxolone methyl DMODA2X Mixed connective tissue disease 4A43.3 Phase 3 [28]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [3]
D(1A) dopamine receptor (DRD1) OTLZPBT7 DRD1_HUMAN Protein Interaction/Cellular Processes [4]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7070).
2 Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates. J Pharm Pharmacol. 2004 Aug;56(8):967-75.
3 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
4 Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects. Arch Gen Psychiatry. 1992 Jul;49(7):538-44. doi: 10.1001/archpsyc.1992.01820070032005.
5 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
6 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
7 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
8 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
9 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
10 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
11 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
12 Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
13 Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
14 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
15 Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
16 Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
17 Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
18 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
19 Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.
20 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
21 Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95.
22 Pergolide is an inhibitor of voltage-gated potassium channels, including Kv1.5, and causes pulmonary vasoconstriction. Circulation. 2005 Sep 6;112(10):1494-9. doi: 10.1161/CIRCULATIONAHA.105.556704. Epub 2005 Aug 29.
23 Dopamine-mediated inhibition of renal Na+/K+-ATPase in HK-2 cells is reduced by ouabain. Clin Exp Pharmacol Physiol. 2010 May;37(5-6):613-8. doi: 10.1111/j.1440-1681.2010.05364.x. Epub 2010 Feb 4.
24 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
25 Characterizing fucoxanthin as a selective dopamine D(3)/D(4) receptor agonist: Relevance to Parkinson's disease. Chem Biol Interact. 2019 Sep 1;310:108757. doi: 10.1016/j.cbi.2019.108757. Epub 2019 Jul 16.
26 Dopamine D1 receptor protein is elevated in nucleus accumbens of human, chronic methamphetamine users. Mol Psychiatry. 2000 Nov;5(6):664-72. doi: 10.1038/sj.mp.4000760.
27 Association study of four dopamine D1 receptor gene polymorphisms and clozapine treatment response. J Psychopharmacol. 2007 Sep;21(7):718-27. doi: 10.1177/0269881106072341. Epub 2006 Nov 8.
28 Characterization of the potent, selective Nrf2 activator, 3-(pyridin-3-ylsulfonyl)-5-(trifluoromethyl)-2H-chromen-2-one, in cellular and in vivo models of pulmonary oxidative stress. J Pharmacol Exp Ther. 2017 Oct;363(1):114-125.