General Information of Drug (ID: DM2HN6Q)

Drug Name
Astemizole Drug Info
Synonyms
Alermizol; Astemina; Astemisan; Astemisol; Astemison; Astemizol; Astemizolum; Astesen; Emdar; Esmacen; Fustermizol; Hestazol; Hismanal; Histamen; Histaminos; Histazol; Hubermizol; Kelp; Laridal; Metodih; Metodik; Paralergin; Retolen; Rifedot; Rimbol; Romadin; Simprox; Urdrim; Wareezol; Waruzol; AlacanBrand of Astemizole; Alonga Brand of Astemizole; Astemizol Alonga; Astemizol [German]; Astemizol ratiopharm; Astemizole Alacan Brand; Astemizole Alonga Brand; Astemizole Byk Brand; Astemizole Diba Brand; Astemizole Elfar Brand; Astemizole Esteve Brand; Astemizole Fustery Brand; Astemizole ICN Brand; Astemizole Janssen Brand; Astemizole Lesvi Brand; Astemizole McNeil Brand; Astemizole Medinsa Brand; Astemizole Merck Brand; Astemizole Senosiain Brand; Astemizole Septa Brand; Astemizole Smaller Brand; Astemizole Urbion Brand; Astemizole Vita Brand; Astemizole ratiopharm Brand; Byk Brand of Astemizole; Diba Brand of Astemizole; Elfar Brand of Astemizole; Esteve Brand of Astemizole; Fustery Brand of Astemizole; ICN Brand of Astemizole; Janssen Brand of Astemizole; Lesvi Brand of Astemizole; McNeil Brand of Astemizole; Medinsa Brand of Astemizole; Merck Brand of Astemizole; Ratiopharm Brand of Astemizole; Reig Jofre Brand of Astemizole; Senosiain Brand of Astemizole; Septa Brand of Astemizole; Smaller Brand of Astemizole; Urbion Brand of Astemizole; Vita Brand of Astemizole; R 42512; [3H]Astemizole; Alonga, Astemizol; Astemizol [INN-Spanish]; Astemizolum [INN-Latin]; HISMANAL (TN); Hismanal (TN); MJD-30; Nono-Nastizol A; Novo-mastizol A; Ratiopharm, Astemizol; Astemizole [USAN:BAN:INN]; GNF-PF-2461; Astemizole (JAN/USP/INN); Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Withdrawn from market [1]
Therapeutic Class
Antiallergic Agents
Cross-matching ID
PubChem CID
2247
ChEBI ID
CHEBI:2896
CAS Number
CAS 68844-77-9
TTD Drug ID
DM2HN6Q
VARIDT Drug ID
DR00705
INTEDE Drug ID
DR0147

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative 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 [15]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [16]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [17]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [18]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [19]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [17]
Doxepin DMPI98T Anxiety Approved [20]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [17]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [21]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [22]
⏷ Show the Full List of 10 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 [23]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [24]
Methotrexate DM2TEOL Anterior urethra cancer Approved [25]
Folic Acid DMEMBJC Colorectal carcinoma Approved [26]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [25]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [25]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [27]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
⏷ 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 [30]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [31]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [32]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [33]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [35]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [36]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [37]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [31]
Verapamil DMA7PEW Angina pectoris BA40 Approved [38]
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [65]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [66]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [67]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [68]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [69]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [69]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [70]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [71]
Capsaicin DMGMF6V Back pain ME84.Z Approved [72]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [73]
⏷ Show the Full List of 20 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 [39]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [40]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [41]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [42]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [43]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [44]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [45]
Propranolol DM79NTF Angina pectoris BA40 Approved [46]
⏷ Show the Full List of 10 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 [47]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [48]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [49]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [6]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [50]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [51]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [52]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [53]
Verapamil DMA7PEW Angina pectoris BA40 Approved [54]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [6]
⏷ 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 [55]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [6]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [6]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [6]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [4]
Verapamil DMA7PEW Angina pectoris BA40 Approved [56]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [6]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [6]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [6]
Metronidazole DMTIVEN Abscess Approved [57]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2J2 (CYP2J2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Riociguat DMXBLMP Chronic thromboembolic pulmonary hypertension Approved [58]
Rivaroxaban DMQMBZ1 Deep vein thrombosis BD71 Approved [59]
Ergocalciferol DMHO0AR Hypoparathyroidism 5A50 Approved [60]
Vorapaxar DMA16BR Myocardial infarction BA41-BA43 Approved [61]
Vitamin D DMWQUC9 N. A. N. A. Approved [60]
Alfacalcidol DM1237M Hyperparathyroidism 5A51 Phase 4 [60]
Ebastine DMH21D9 N. A. N. A. Phase 4 [7]
MANIDIPINE DMJPGUA N. A. N. A. Phase 3 [62]
Carebastine DMUVMWZ Ocular allergy 4A81 Phase 3 [63]
Eperisone DM1SMAI Muscle spasm MB47.3 Phase 3 [64]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [62]
Quercetin DM3NC4M Obesity 5B81 Approved [74]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [75]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [76]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [77]
Nisoldipine DM7ISKJ Hypertension BA00-BA04 Approved [62]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [78]
Amlodipine DMBDAZV Angina pectoris BA40 Approved [62]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [79]
Gemfibrozil DMD8Q3J Hyperlipidaemia 5C80 Approved [80]
⏷ Show the Full List of 20 Drug(s)
Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [81]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [8]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [8]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [82]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [81]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [8]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [83]
Gefitinib DM15F0X Colon adenocarcinoma Approved [81]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [84]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [81]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [85]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [86]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [87]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [88]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [85]
Resveratrol DM3RWXL Giant cell arteritis 4A44.2 Phase 3 [89]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [90]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [91]
Desmethylastemizole DM58XJN Discovery agent N.A. Investigative [92]
⏷ Show the Full List of 9 Drug(s)
Drug(s) Affected By Metallothionein-2 (MT2A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [93]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [94]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [95]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [9]
Quercetin DM3NC4M Obesity 5B81 Approved [96]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [97]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y Approved [98]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [99]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [100]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [101]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Heme oxygenase 1 (HMOX1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [102]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [103]
Pantothenic acid DM091H2 Vitamin deficiency 5B55-5B71 Approved [104]
Verapamil DMA7PEW Angina pectoris BA40 Approved [105]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [106]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [107]
Selenium DM25CGV N. A. N. A. Approved [108]
TECFIDERA DM2OVDT Multiple sclerosis 8A40 Approved [109]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [110]
Methotrexate DM2TEOL Anterior urethra cancer Approved [111]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [112]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [113]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [107]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [114]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [115]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [116]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [117]
Leflunomide DMR8ONJ Arthritis FA20 Approved [118]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [78]
Testosterone enanthate DMB6871 N. A. N. A. Approved [119]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [103]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [95]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [120]
Methotrexate DM2TEOL Anterior urethra cancer Approved [121]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [122]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [9]
Quercetin DM3NC4M Obesity 5B81 Approved [74]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [123]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [116]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y 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 [124]
Quinidine DMLPICK N. A. N. A. Approved [125]
Verapamil DMA7PEW Angina pectoris BA40 Approved [126]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [127]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [127]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [128]
Propranolol DM79NTF Angina pectoris BA40 Approved [129]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [130]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [131]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [127]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Metallothionein-1M (MT1M)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [103]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [9]
Quercetin DM3NC4M Obesity 5B81 Approved [74]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [132]
Phenoxybenzamine DM8KSQH Malignant essential hypertension BA00 Approved [9]
Leflunomide DMR8ONJ Arthritis FA20 Approved [118]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [78]
Disulfiram DMCL2OK Alcohol dependence 6C40.2 Approved [9]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [86]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [133]
⏷ 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
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_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 [6]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [6]
Cytochrome P450 2J2 (CYP2J2) DERSX5P CP2J2_HUMAN Substrate [7]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [8]
Cyclic AMP-dependent transcription factor ATF-3 (ATF3) OTC1UOHP ATF3_HUMAN Gene/Protein Processing [9]
Cytochrome P450 2J2 (CYP2J2) OTJBTEH8 CP2J2_HUMAN Biotransformations [10]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Regulation of Drug Effects [11]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Gene/Protein Processing [9]
Metallothionein-1M (MT1M) OTVT8PLU MT1M_HUMAN Gene/Protein Processing [9]
Metallothionein-2 (MT2A) OTHOACHD MT2_HUMAN Gene/Protein Processing [9]
Microtubule-associated protein tau (MAPT) OTMTP2Z7 TAU_HUMAN Protein Interaction/Cellular Processes [12]
Potassium voltage-gated channel subfamily H member 1 (KCNH1) OTZZXWER KCNH1_HUMAN Gene/Protein Processing [13]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [14]

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: 2603).
2 Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12.
3 Improving the prediction of the brain disposition for orally administered drugs using BDDCS. Adv Drug Deliv Rev. 2012 Jan;64(1):95-109.
4 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
5 Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine. Br J Clin Pharmacol. 2001 Feb;51(2):133-42.
6 Drug Interactions Flockhart Table
7 Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51.
8 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
9 Identification of novel activators of the metal responsive transcription factor (MTF-1) using a gene expression biomarker in a microarray compendium. Metallomics. 2020 Sep 23;12(9):1400-1415. doi: 10.1039/d0mt00071j.
10 Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole. Drug Metab Dispos. 2002 Nov;30(11):1240-5.
11 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.
12 Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease. J Alzheimers Dis. 2010;19(2):573-89. doi: 10.3233/JAD-2010-1262.
13 Functional and molecular identification of intermediate-conductance Ca(2+)-activated K(+) channels in breast cancer cells: association with cell cycle progression. Am J Physiol Cell Physiol. 2004 Jul;287(1):C125-34. doi: 10.1152/ajpcell.00488.2003. Epub 2004 Feb 25.
14 Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel. Eur J Pharmacol. 1999 Jun 25;374(3):457-60. doi: 10.1016/s0014-2999(99)00375-1.
15 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
16 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.
17 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.
18 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
19 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
20 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
21 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.
22 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
23 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
24 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
25 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.
26 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
27 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
28 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
29 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.
30 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.
31 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
32 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.
33 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
34 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.
35 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.
36 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
37 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.
38 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.
39 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
40 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.
41 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
42 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.
43 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
44 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
45 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
46 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
47 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.
48 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.
49 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.
50 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.
51 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
52 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
53 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
54 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
55 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.
56 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
57 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.
58 Riociguat (adempas): a novel agent for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. P T. 2014 Nov;39(11):749-58.
59 Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85.
60 Characterization of rat and human CYP2J enzymes as Vitamin D 25-hydroxylases. Steroids. 2006 Oct;71(10):849-56.
61 Vorapaxar: the missing link in antiplatelet therapy! J Anaesthesiol Clin Pharmacol. 2017 Apr-Jun;33(2):269-270.
62 Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine. Chem Biol Interact. 2019 Jun 1;306:1-9.
63 Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A. Drug Metab Dispos. 2006 Nov;34(11):1793-7.
64 Characterization of human cytochrome P450 enzymes involved in the biotransformation of eperisone. Xenobiotica. 2009 Jan;39(1):1-10.
65 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
66 Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
67 Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
68 The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
69 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.
70 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
71 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
72 Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
73 Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
74 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.
75 In vitro inhibition of human small intestinal and liver microsomal astemizole O-demethylation: different contribution of CYP2J2 in the small intestine and liver. Xenobiotica. 2003 Jun;33(6):615-23.
76 Differentiation-specific factors modulate epidermal CYP1-4 gene expression in human skin in response to retinoic acid and classic aryl hydrocarbon receptor ligands. J Pharmacol Exp Ther. 2006 Dec;319(3):1162-71.
77 Cytochrome P450 expression, induction and activity in human induced pluripotent stem cell-derived intestinal organoids and comparison with primary human intestinal epithelial cells and Caco-2 cells. Arch Toxicol. 2021 Mar;95(3):907-922. doi: 10.1007/s00204-020-02953-6. Epub 2020 Dec 2.
78 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
79 Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
80 Expression of cytochrome P450 epoxygenases and soluble epoxide hydrolase is regulated by hypolipidemic drugs in dose-dependent manner. Toxicol Appl Pharmacol. 2018 Sep 15;355:156-163.
81 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
82 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
83 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.
84 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
85 Estrogens and human papilloma virus oncogenes regulate human ether--go-go-1 potassium channel expression. Cancer Res. 2009 Apr 15;69(8):3300-7. doi: 10.1158/0008-5472.CAN-08-2036. Epub 2009 Apr 7.
86 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.
87 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
88 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
89 A novel long noncoding RNA AK001796 acts as an oncogene and is involved in cell growth inhibition by resveratrol in lung cancer. Toxicol Appl Pharmacol. 2015 Jun 1;285(2):79-88.
90 Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma. Oncotarget. 2014 May 15;5(9):2355-71.
91 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
92 A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. doi: 10.1038/nchembio806. Epub 2006 Jul 2.
93 Expression pattern of cisplatin-induced metallothionein isoforms in squamous cell carcinoma. Anticancer Res. 2003 Jan-Feb;23(1A):299-303.
94 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
95 Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
96 Expression of antioxidant proteins in human intestinal Caco-2 cells treated with dietary flavonoids. Cancer Lett. 1999 Nov 15;146(2):161-7.
97 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
98 Motexafin gadolinium and zinc induce oxidative stress responses and apoptosis in B-cell lymphoma lines. Cancer Res. 2005 Dec 15;65(24):11676-88.
99 Chronic occupational exposure to arsenic induces carcinogenic gene signaling networks and neoplastic transformation in human lung epithelial cells. Toxicol Appl Pharmacol. 2012 Jun 1;261(2):204-16.
100 JunD is involved in the antiproliferative effect of Delta9-tetrahydrocannabinol on human breast cancer cells. Oncogene. 2008 Aug 28;27(37):5033-44.
101 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
102 Dexamethasone and the inflammatory response in explants of human omental adipose tissue. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):292-8.
103 Inhibiting Heat Shock Proteins Can Potentiate the Cytotoxic Effect of Cannabidiol in Human Glioma Cells. Anticancer Res. 2015 Nov;35(11):5827-37.
104 Calcium pantothenate modulates gene expression in proliferating human dermal fibroblasts. Exp Dermatol. 2009 Nov;18(11):969-78. doi: 10.1111/j.1600-0625.2009.00884.x. Epub 2009 Apr 8.
105 Protective role of HO-1 for alcohol-dependent liver damage. Dig Dis. 2010;28(6):792-8. doi: 10.1159/000324287. Epub 2011 Apr 27.
106 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
107 Neuroprotective effects of glucomoringin-isothiocyanate against H(2)O(2)-Induced cytotoxicity in neuroblastoma (SH-SY5Y) cells. Neurotoxicology. 2019 Dec;75:89-104. doi: 10.1016/j.neuro.2019.09.008. Epub 2019 Sep 12.
108 High selenium status in individuals exposed to arsenic through coal-burning in Shaanxi (PR of China) modulates antioxidant enzymes, heme oxygenase-1 and DNA damage. Clin Chim Acta. 2010 Sep 6;411(17-18):1312-8.
109 Dimethyl Fumarate Inhibits the Nuclear Factor B Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein. J Biol Chem. 2016 Feb 12;291(7):3639-47. doi: 10.1074/jbc.M115.679704. Epub 2015 Dec 18.
110 Combination treatment with arsenic trioxide and sulindac enhances apoptotic cell death in lung cancer cells via activation of oxidative stress and mitogen-activated protein kinases. Oncol Rep. 2008 Aug;20(2):379-84.
111 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
112 Cannabidiol Modulates the Expression of Alzheimer's Disease-Related Genes in Mesenchymal Stem Cells. Int J Mol Sci. 2016 Dec 23;18(1):26. doi: 10.3390/ijms18010026.
113 The estrogen receptor influences microtubule-associated protein tau (MAPT) expression and the selective estrogen receptor inhibitor fulvestrant downregulates MAPT and increases the sensitivity to taxane in breast cancer cells. Breast Cancer Res. 2010;12(3):R43. doi: 10.1186/bcr2598. Epub 2010 Jun 28.
114 Pharmacologic reductions of total tau levels; implications for the role of microtubule dynamics in regulating tau expression. Mol Neurodegener. 2006 Jul 26;1:6. doi: 10.1186/1750-1326-1-6.
115 Differential effects of simvastatin and pravastatin on expression of Alzheimer's disease-related genes in human astrocytes and neuronal cells. J Lipid Res. 2009 Oct;50(10):2095-102. doi: 10.1194/jlr.M900236-JLR200. Epub 2009 May 21.
116 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.
117 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
118 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
119 Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
120 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
121 Development and validation of the TGx-HDACi transcriptomic biomarker to detect histone deacetylase inhibitors in human TK6 cells. Arch Toxicol. 2021 May;95(5):1631-1645. doi: 10.1007/s00204-021-03014-2. Epub 2021 Mar 26.
122 Simvastatin inactivates beta1-integrin and extracellular signal-related kinase signaling and inhibits cell proliferation in head and neck squamous cell carcinoma cells. Cancer Sci. 2007 Jun;98(6):890-9.
123 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
124 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.
125 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.
126 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.
127 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.
128 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.
129 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.
130 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.
131 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.
132 Global effects of inorganic arsenic on gene expression profile in human macrophages. Mol Immunol. 2009 Feb;46(4):649-56.
133 Identification of mechanisms of action of bisphenol a-induced human preadipocyte differentiation by transcriptional profiling. Obesity (Silver Spring). 2014 Nov;22(11):2333-43.