General Information of Drug (ID: DM24XYQ)

Drug Name
Bromperidol Drug Info
Synonyms
bromperidol; 10457-90-6; Impromen; Bromoperidol; Tesoprel; Azurene; 4-(4-(4-bromophenyl)-4-hydroxypiperidin-1-yl)-1-(4-fluorophenyl)butan-1-one; UNII-LYH6F7I22E; Bromperidolum [INN-Latin]; R 11333; EINECS 233-943-3; 4-(4-(4-Bromophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone; CC 2489; BRN 1552256; LYH6F7I22E; 4-(4-(p-Bromophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone; RKLNONIVDFXQRX-UHFFFAOYSA-N; 4-(4-(4-Bromophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone; NCGC00016692-01; CAS-10457-90-6
Indication
Disease Entry ICD 11 Status REF
Schizophrenia 6A20 Approved [1]
Cross-matching ID
PubChem CID
2448
ChEBI ID
CHEBI:31305
CAS Number
CAS 10457-90-6
TTD Drug ID
DM24XYQ
INTEDE Drug ID
DR0236

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DME
DOT
Drug Status:
Approved Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [6]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [7]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [8]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [9]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [10]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [11]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [12]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [13]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [7]
Verapamil DMA7PEW Angina pectoris BA40 Approved [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Vidarabine DM0N85H Hepatosplenic T-cell lymphoma Approved [4]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [15]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [16]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [17]
Etidronic acid DM1XHYJ Bone Paget disease Approved [4]
Tiaprofenic acid DM23D7J Osteoarthritis FA00-FA05 Approved [4]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [18]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [19]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [21]
Quinidine DMLPICK N. A. N. A. Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [24]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [24]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [25]
Propranolol DM79NTF Angina pectoris BA40 Approved [26]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [27]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [28]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [24]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By D(2) dopamine receptor (DRD2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Droperidol DM0DXA8 Nausea MD90 Approved [29]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [29]
Zuclopenthixol DMKYD5N Schizophrenia 6A20 Approved [29]
Meglitinides DM1OFHN Type-2 diabetes 5A11 Approved [30]
Sulpiride DMF54ZG Schizophrenia 6A20 Approved [31]
Risperidone DMN6DXL Bipolar I disorder Approved [32]
Olanzapine DMPFN6Y Bipolar depression Approved [33]
Methamphetamine DMPM4SK Anxiety Approved [34]
Bromocriptine DMVE3TK Acromegaly 5A60.0 Approved [35]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [36]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
D(2) dopamine receptor (DRD2) OTBLXKEG DRD2_HUMAN Drug Response [3]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Gene/Protein Processing [4]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [5]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 CYP3A is responsible for N-dealkylation of haloperidol and bromperidol and oxidation of their reduced forms by human liver microsomes. Life Sci. 2000 Nov 3;67(24):2913-20.
3 The -141C Ins/Del polymorphism in the dopamine D2 receptor gene promoter region is associated with anxiolytic and antidepressive effects during treatment with dopamine antagonists in schizophrenic patients. Pharmacogenetics. 2001 Aug;11(6):545-50. doi: 10.1097/00008571-200108000-00009.
4 Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. Toxicol Lett. 2015 Jan 5;232(1):193-202. doi: 10.1016/j.toxlet.2014.10.009. Epub 2014 Oct 16.
5 Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
6 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
7 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
8 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
9 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
10 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
11 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
12 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
13 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
14 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
15 Induction of PXR-mediated metabolism by beta-carotene. Biochim Biophys Acta. 2005 May 30;1740(2):162-9. doi: 10.1016/j.bbadis.2004.11.013. Epub 2004 Dec 8.
16 Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR). Toxicol Appl Pharmacol. 2005 Dec 1;209(2):123-33. doi: 10.1016/j.taap.2005.03.015.
17 Identification and validation of novel human pregnane X receptor activators among prescribed drugs via ligand-based virtual screening. Drug Metab Dispos. 2011 Feb;39(2):337-44. doi: 10.1124/dmd.110.035808. Epub 2010 Nov 10.
18 Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9.
19 Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of pregnane X (PXR) receptor. Toxicol Lett. 2017 Jan 4;265:86-96.
20 Stable cellular models of nuclear receptor PXR for high-throughput evaluation of small molecules. Toxicol In Vitro. 2018 Oct;52:222-234.
21 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
22 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
23 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
24 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
25 Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
26 Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
27 Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
28 Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.
29 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.
30 Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia. Psychopharmacology (Berl). 2008 Apr;197(2):229-35. doi: 10.1007/s00213-007-1029-z. Epub 2007 Dec 6.
31 Positron emission tomography measurement of dopamine D? receptor occupancy in the pituitary and cerebral cortex: relation to antipsychotic-induced hyperprolactinemia. J Clin Psychiatry. 2010 Sep;71(9):1131-7. doi: 10.4088/JCP.08m04307yel. Epub 2010 Feb 23.
32 Variants of the dopamine D2 receptor gene and risperidone-induced hyperprolactinemia in children and adolescents. Pharmacogenet Genomics. 2009 May;19(5):373-82. doi: 10.1097/FPC.0b013e328329a60f.
33 Dopamine receptor D2 gene is associated with weight gain in schizophrenic patients under long-term atypical antipsychotic treatment. Pharmacogenet Genomics. 2010 Jun;20(6):359-66. doi: 10.1097/FPC.0b013e3283397d06.
34 A preliminary study: novelty seeking, frontal executive function, and dopamine receptor (D2) TaqI A gene polymorphism in patients with methamphetamine dependence. Compr Psychiatry. 2008 Jul-Aug;49(4):387-92. doi: 10.1016/j.comppsych.2008.01.008. Epub 2008 Mar 21.
35 Imaging gene-substance interactions: the effect of the DRD2 TaqIA polymorphism and the dopamine agonist bromocriptine on the brain activation during the anticipation of reward. Neurosci Lett. 2006 Sep 25;405(3):196-201. doi: 10.1016/j.neulet.2006.07.030. Epub 2006 Aug 8.
36 Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. doi: 10.1073/pnas.0609752104. Epub 2007 Jul 2.