General Information of Drug (ID: DMJSKUI)

Drug Name
Norcisapride Drug Info
Synonyms
Norcisapride; 84946-16-7; CHEMBL1748; 4-Amino-5-chloro-2-methoxy-N-(3-methoxy-4-piperidyl)benzamide; 4-amino-5-chloro-2-methoxy-N-(3-methoxy-4-piperidinyl)benzamide; (4-Amino-5-chloro-2-methoxy)-N-[3-methoxy(4-piperidyl)]benzamide; 4-amino-5-chloro-2-methoxy-N-(3-methoxypiperidin-4-yl)benzamide; Benzamide,4-amino-5-chloro-2-methoxy-N-[(3S,4R)-3-methoxy-4-piperidinyl]-, hydrochloride(1:1); EINECS 284-619-3; AC1MI81F; SCHEMBL593405; CTK4E8653; OMLDMGPCWMBPAN-UHFFFAOYSA-N; BDBM50301927; AKOS030254741; API0006151; DB-076176
Indication
Disease Entry ICD 11 Status REF
Gastroesophageal reflux disease DA22.Z Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
3019427
CAS Number
CAS 84946-16-7
TTD Drug ID
DMJSKUI
INTEDE Drug ID
DR1780

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Drug(s) Targeting 5-HT 4 receptor (HTR4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisapride DMY7PED Gastroesophageal reflux disease DA22.Z Approved [4]
Tegaserod DM3XYD1 Irritable bowel syndrome DD91.0 Approved [5]
R0-93877 DMM4U9G Constipation DD91.1 Approved [6]
HTF 919 DM78G6F Constipation DD91.1 Approved [7]
Mosapride DM2VOQ3 N. A. N. A. Phase 4 [8]
Renzapride DM7HQNX Irritable bowel syndrome DD91.0 Phase 3 [9]
Lintopride DMSHGWN Nausea MD90 Phase 2 [10]
TD-8954 DM3C9NV Gastrointestinal disease DE2Z Phase 2 [11]
SB-207266A DM27KFY Irritable bowel syndrome DD91.0 Phase 2 [6]
YKP-GI DM740LV Constipation DD91.1 Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 3A receptor (HTR3A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dolasetron DMMG26Z Nausea MD90 Approved [13]
Alosetron DML2A03 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [14]
Tropisetron DMNSJ7V Fibromyalgia MG30.01 Approved [15]
Palonosetron DMBHMOX Nausea MD90 Approved [16]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [15]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [17]
Cilansetron DMP0NGX Irritable bowel syndrome DD91.0 Phase 3 [18]
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [19]
YM-114 DML2IXO Nausea MD90 Discontinued in Phase 2 [20]
ATI-17000 DMZJVR5 Irritable bowel syndrome DD91.0 Preclinical [5]
⏷ 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 [21]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [22]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [23]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [24]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [27]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [28]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [29]
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [30]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [31]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [32]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [33]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [34]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [34]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [35]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [36]
Capsaicin DMGMF6V Back pain ME84.Z Approved [37]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [38]
⏷ Show the Full List of 20 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Inhibitor [2]
5-HT 4 receptor (HTR4) TT07C3Y 5HT4R_HUMAN Inhibitor [2]

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

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Biotransformations [3]

References

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11 The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011 May 30;2:25.
12 A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015 Apr;13(4):701-8.e1.
13 Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, do... Lancet Oncol. 2009 Feb;10(2):115-24.
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16 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
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21 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.
22 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
23 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.
24 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
25 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.
26 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.
27 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
28 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.
29 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.
30 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
31 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.
32 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.
33 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.
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36 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
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38 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.