General Information of Drug (ID: DM5URA2)

Drug Name
Chlorpheniramine Drug Info
Synonyms
Allergican; Allergisan; Antagonate; Chloropheniramine; Chlorophenylpyridamin; Chlorophenylpyridamine; Chloropiril; Chloroprophenpyridamine; Chlorphenamine; Chlorphenaminum; Chlorpheniraminum; Chlorprophenpyridamine; Clofeniramina; Clorfenamina; Clorfeniramina; Cloropiril; Haynon; Hayon; Histadur; ISOCLOR; Kloromin; Phenetron; PiriIton; Piriton; Polaronil; Telachlor; Teldrin; Chlorphenamine [INN]; Clorfeniramina [Italian]; Pediacare Allergy Formula; [3H]Chlorpheniramine; Aller-Chlor; Chlo-amine; Chlor-Pro; Chlor-Trimeton Repetabs; Chlor-trimeton; Chlorphenamine (INN); Chlorphenaminum [INN-Latin]; Clofeniramina (TN); Clorfenamina [INN-Spanish]; Comakin (TN); Gen-Allerate; Novo-Pheniram; Piriton (TN); Chlor-Trimeton (TN); Chlor-Tripolon (TN); CHLORPHENIRAMINE (SEE ALSO: CHLORPHENIRAMINE MALEATE (CAS113-92-8)); Gamma-(4-Chlorophenyl)-gamma-(2-pyridyl)propyldimethylamine; Gamma-(4-Chlorophenyl)-N,N-dimethyl-2-pyridinepropanamine; 1-(p-Chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine; 1-(p-Chlorophenyl)-1-(2-pyridyl)-3-dimethylaminopropane; 2-(p-Chloro-alpha-(2-(dimethylamino)ethyl)benzyl)pyridine; 3-(4-chlorophenyl)-N,N-dimethyl-3-(pyridin-2-yl)propan-1-amine; 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine; 3-(p-Chlorophenyl)-3-(2-pyridyl)-N,N-dimethylpropylamine; 4-Chloropheniramine
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1]
Therapeutic Class
Antiallergic Agents
Cross-matching ID
PubChem CID
2725
ChEBI ID
CHEBI:52010
CAS Number
CAS 113-92-8
TTD Drug ID
DM5URA2
VARIDT Drug ID
DR00595
INTEDE Drug ID
DR0304
ACDINA Drug ID
D00123

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Histamine H1 receptor (H1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [13]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [14]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [2]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [15]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [16]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [2]
Doxepin DMPI98T Anxiety Approved [17]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [18]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [19]
Tranilast DME5Y64 Allergic rhinitis CA08.0 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [21]
Methotrexate DM2TEOL Anterior urethra cancer Approved [22]
Folic Acid DMEMBJC Colorectal carcinoma Approved [23]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [24]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [26]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [27]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [28]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [29]
Daunorubicin DMQUSBT Acute monocytic leukemia Approved [30]
⏷ Show the Full List of 10 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 [31]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [32]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [33]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [34]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [35]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [36]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [37]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [38]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [32]
Verapamil DMA7PEW Angina pectoris BA40 Approved [39]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [40]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [41]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [42]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [35]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [39]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [43]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [44]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [45]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [46]
Propranolol DM79NTF Angina pectoris BA40 Approved [47]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [60]
Paliperidone DM7NPJS Psychotic disorder 6A20-6A25 Approved [61]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [62]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [63]
Oxatomide DM1F42Z Hay fever CA08.00 Approved [64]
Cinacalcet DMCX0K3 Hyperparathyroidism 5A51 Approved [65]
Capsaicin DMGMF6V Back pain ME84.Z Approved [66]
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [67]
Quinidine DMLPICK N. A. N. A. Approved [68]
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [69]
⏷ Show the Full List of 20 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [48]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [49]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [50]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [4]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [51]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [52]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [53]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [54]
Verapamil DMA7PEW Angina pectoris BA40 Approved [55]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [4]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A7 (CYP3A7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [56]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [4]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [4]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [4]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [57]
Verapamil DMA7PEW Angina pectoris BA40 Approved [58]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [4]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [4]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [4]
Metronidazole DMTIVEN Abscess Approved [59]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cholinesterase (BCHE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [70]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [71]
Galantamine DMEO794 Alzheimer disease 8A20 Approved [72]
Rivastigmine DMG629M Alzheimer disease 8A20 Approved [73]
Donepezil DMIYG7Z Advanced cancer 2A00-2F9Z Approved [74]
Succinylcholine DM2ET1M Plasma cell myeloma 2A83.1 Approved [75]
Ethopropazine DM0N3L7 Parkinson disease 8A00.0 Approved [71]
Dimenhydrinate DM264B3 Meniere disease AB31.0 Approved [6]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [76]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [77]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tolbutamide DM02AWV Advanced cancer 2A00-2F9Z Approved [12]
Diazepam DM08E9O Alcohol withdrawal Approved [12]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [78]
Selenium DM25CGV N. A. N. A. Approved [79]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [12]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [12]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [12]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [12]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [12]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [80]
Verapamil DMA7PEW Angina pectoris BA40 Approved [81]
Methysergide DM1EF73 Migraine 8A80 Approved [9]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [82]
Methotrexate DM2TEOL Anterior urethra cancer Approved [83]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [9]
Quercetin DM3NC4M Obesity 5B81 Approved [84]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [85]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [86]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [87]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Hypertriglyceridemia 5C80.1 Approved [88]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [89]
Gamolenic acid DMQN30Z Allergy 4A80-4A85 Approved [90]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [91]
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [92]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [93]
Ibandronate DM0QZBN Hypercalcaemia 5B91.0 Approved [94]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [95]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [96]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [97]
SPI-1005 DM6XFHS Reperfusion injury ND56.Z Approved [8]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [8]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [98]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [99]
Ceftazidime DM41GRA Bacteremia 1A73 Approved [8]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [100]
Ethacrynic acid DM60QMR Edema MG29 Approved [8]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [8]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [98]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [101]
Quinidine DMLPICK N. A. N. A. Approved [102]
Verapamil DMA7PEW Angina pectoris BA40 Approved [103]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [104]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [104]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [105]
Propranolol DM79NTF Angina pectoris BA40 Approved [106]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [107]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [108]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [104]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 1 (ABCC1) DTSYQGK MRP1_HUMAN Substrate [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [5]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [4]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cholinesterase (BCHE) OTOH3WQ9 CHLE_HUMAN Gene/Protein Processing [6]
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Drug Response [7]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Gene/Protein Processing [8]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Gene/Protein Processing [9]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [10]
Prostaglandin G/H synthase 2 (PTGS2) OT75U9M4 PGH2_HUMAN Gene/Protein Processing [11]
Transmembrane protease serine 2 (TMPRSS2) OTN44YQ5 TMPS2_HUMAN Gene/Protein Processing [12]

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: 6976).
2 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
3 Carrier mediated transport of chlorpheniramine and chlorcyclizine across bovine olfactory mucosa: implications on nose-to-brain transport. J Pharm Sci. 2005 Mar;94(3):613-24.
4 Drug Interactions Flockhart Table
5 The roles of CYP2D6 and stereoselectivity in the clinical pharmacokinetics of chlorpheniramine. Br J Clin Pharmacol. 2002 May;53(5):519-25.
6 Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: analysis of its postulated role in synergizing organophosphate toxicity. Toxicol Appl Pharmacol. 1975 Feb;31(2):179-90.
7 Impact of CYP2D6*10 on H1-antihistamine-induced hypersomnia. Eur J Clin Pharmacol. 2006 Dec;62(12):995-1001. doi: 10.1007/s00228-006-0210-3. Epub 2006 Nov 7.
8 A Gene Expression Biomarker Predicts Heat Shock Factor 1 Activation in a Gene Expression Compendium. Chem Res Toxicol. 2021 Jul 19;34(7):1721-1737. doi: 10.1021/acs.chemrestox.0c00510. Epub 2021 Jun 25.
9 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
10 Block of HERG k channel by classic histamine h(1) receptor antagonist chlorpheniramine. Korean J Physiol Pharmacol. 2009 Jun;13(3):215-20. doi: 10.4196/kjpp.2009.13.3.215. Epub 2009 Jun 30.
11 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
12 Effect of common medications on the expression of SARS-CoV-2 entry receptors in liver tissue. Arch Toxicol. 2020 Dec;94(12):4037-4041. doi: 10.1007/s00204-020-02869-1. Epub 2020 Aug 17.
13 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
14 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
15 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
16 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
17 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
18 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
19 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
20 Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
21 The role of bioreductive activation of doxorubicin in cytotoxic activity against leukaemia HL60-sensitive cell line and its multidrug-resistant sublines. Br J Cancer. 2005 Jul 11;93(1):89-97.
22 Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32.
23 Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
24 Hammerhead ribozyme against gamma-glutamylcysteine synthetase sensitizes human colonic cancer cells to cisplatin by down-regulating both the glutathione synthesis and the expression of multidrug resistance proteins. Cancer Gene Ther. 2001 Oct;8(10):803-14.
25 Multidrug resistance-associated protein-1 functional activity in Calu-3 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1199-205.
26 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
27 ATP-Dependent efflux of CPT-11 and SN-38 by the multidrug resistance protein (MRP) and its inhibition by PAK-104P. Mol Pharmacol. 1999 May;55(5):921-8.
28 Structural determinants of substrate specificity differences between human multidrug resistance protein (MRP) 1 (ABCC1) and MRP3 (ABCC3). Drug Metab Dispos. 2008 Dec;36(12):2571-81.
29 Evaluation of transport of common antiepileptic drugs by human multidrug resistance-associated proteins (MRP1, 2 and 5) that are overexpressed in pharmacoresistant epilepsy. Neuropharmacology. 2010 Jun;58(7):1019-32.
30 Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83.
31 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.
32 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
33 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.
34 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
35 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.
36 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.
37 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
38 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.
39 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.
40 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
41 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
42 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
43 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
44 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
45 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
46 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
47 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
48 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
49 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
50 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
51 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
52 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
53 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
54 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
55 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
56 The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
57 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
58 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
59 The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
60 Human recombinant cytochrome P450 enzymes display distinct hydrogen peroxide generating activities during substrate independent NADPH oxidase reactions. Toxicol Sci. 2014 Oct;141(2):344-52. doi: 10.1093/toxsci/kfu133. Epub 2014 Jul 24.
61 Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology (Berl). 1999 Dec;147(3):300-5. doi: 10.1007/s002130051171.
62 Effect of penicillin-based antibiotics, amoxicillin, ampicillin, and piperacillin, on drug-metabolizing activities of human hepatic cytochromes P450. J Toxicol Sci. 2016 Feb;41(1):143-6.
63 Cannabidiol, a major phytocannabinoid, as a potent atypical inhibitor for CYP2D6. Drug Metab Dispos. 2011 Nov;39(11):2049-56. doi: 10.1124/dmd.111.041384. Epub 2011 Aug 5.
64 Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants. Biol Pharm Bull. 2005 Feb;28(2):328-34.
65 Pharmacokinetics of desipramine HCl when administered with cinacalcet HCl. Eur J Clin Pharmacol. 2007 Feb;63(2):159-63.
66 Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo. J Asian Nat Prod Res. 2012;14(4):382-95.
67 Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
68 Inhibition of cytochrome P4502D6 activity with paroxetine normalizes the ultrarapid metabolizer phenotype as measured by nortriptyline pharmacokinetics and the debrisoquin test. Clin Pharmacol Ther. 2001 Oct;70(4):327-35.
69 Interaction of buprenorphine and its metabolite norbuprenorphine with cytochromes p450 in vitro. Drug Metab Dispos. 2003 Jun;31(6):768-72.
70 Increased organophosphate scavenging in a butyrylcholinesterase mutant. Chem Biol Interact. 2008 Sep 25;175(1-3):376-9. doi: 10.1016/j.cbi.2008.04.012. Epub 2008 Apr 22.
71 Comparative effects of cationic triarylmethane, phenoxazine and phenothiazine dyes on horse serum butyrylcholinesterase. Arch Biochem Biophys. 2008 Oct 15;478(2):201-5.
72 Lichens of parmelioid clade as promising multitarget neuroprotective agents. Chem Res Toxicol. 2019 Jun 17;32(6):1165-1177.
73 Potencies and selectivities of inhibitors of acetylcholinesterase and its molecular forms in normal and Alzheimer's disease brain. Acta Biol Hung. 2003;54(2):183-9. doi: 10.1556/ABiol.54.2003.2.7.
74 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.
75 Response of the newborn to succinlycholine injection in homozygotic atypical mothers. Anesthesiology. 1975 Jul;43(1):115-6. doi: 10.1097/00000542-197507000-00028.
76 Qualitative defects of pseudocholinesterase activity. Anaesthesia. 1967 Jan;22(1):55-68.
77 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
78 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
79 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
80 [Reversal effect of MDR1 and MDR3 gene silencing on resistance of A2780/taxol cells to paclitaxel]. Zhonghua Fu Chan Ke Za Zhi. 2007 Jun;42(6):412-6.
81 8-Methoxypsoralen disrupts MDR3-mediated phospholipids efflux and bile acid homeostasis and its relevance to hepatotoxicity. Toxicology. 2017 Jul 1;386:40-48. doi: 10.1016/j.tox.2017.05.011. Epub 2017 May 24.
82 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
83 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
84 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
85 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
86 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
87 Evaluation of gene induction of drug-metabolizing enzymes and transporters in primary culture of human hepatocytes using high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi. 2002 May;122(5):339-61.
88 Docosahexaenoic acid regulates gene expression in HUVEC cells treated with polycyclic aromatic hydrocarbons. Toxicol Lett. 2015 Jul 16;236(2):75-81.
89 Etoposide induces necrosis through p53-mediated antiapoptosis in human kidney proximal tubule cells. Toxicol Sci. 2015 Nov;148(1):204-19.
90 Conjugated linoleic acid, unlike other unsaturated fatty acids, strongly induces glutathione synthesis without any lipoperoxidation. Br J Nutr. 2006 Nov;96(5):811-9.
91 COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
92 Mitochondrial involvement in schizophrenia and other functional psychoses. Neurochem Res. 1996 Sep;21(9):995-1004.
93 Immunomodulatory effect of selective serotonin reuptake inhibitors (SSRIs) on human T lymphocyte function and gene expression. Eur Neuropsychopharmacol. 2007 Dec;17(12):774-80.
94 Stimulation of cyclooxygenase-2 expression by bone-derived transforming growth factor-beta enhances bone metastases in breast cancer. Cancer Res. 2006 Feb 15;66(4):2067-73.
95 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
96 A2E selectively induces cox-2 in ARPE-19 and human neural cells. Curr Eye Res. 2006 Mar;31(3):259-63.
97 NRF2 transcriptionally activates the heat shock factor 1 promoter under oxidative stress and affects survival and migration potential of MCF7 cells. J Biol Chem. 2018 Dec 14;293(50):19303-19316. doi: 10.1074/jbc.RA118.003376. Epub 2018 Oct 11.
98 Non-steroidal anti-inflammatory drugs inhibit the expression of cytokines and induce HSP70 in human monocytes. Cytokine. 1999 May;11(5):347-58. doi: 10.1006/cyto.1998.0437.
99 Simvastatin induces heat shock factor 1 in vascular endothelial cells. Atherosclerosis. 2006 Oct;188(2):265-73. doi: 10.1016/j.atherosclerosis.2005.10.045. Epub 2005 Dec 20.
100 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
101 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.
102 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.
103 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.
104 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.
105 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.
106 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.
107 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.
108 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.