Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMDPM7R)

• Drug Name: Y-25130 Drug Info
• Synonyms: Azasetron; Nazasetron; Azasetron [INN]; C17H20ClN3O3; 123039-99-6; WUKZPHOXUVCQOR-UHFFFAOYSA-N; Azasetron (INN); 6-Chloro-4-methyl-3-oxo-N-(quinuclidin-3-yl)-3,4-dihydro-2H-benzo[b][1,4]oxazine-8-carboxamide; NCGC00024563-02; DSSTox_RID_81029; DSSTox_CID_25651; DSSTox_GSID_45651; (- )-6-Chloro-3,4-dihydro-4-methyl-3-oxo-N-3-quinuclidinyl-2H-1,4-benzoxazine-8-carboxamide; N-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide

Indication

Disease Entry	ICD 11	Status	REF
Nausea and vomiting	MD90	Approved	[1]

• Cross-matching ID:
  PubChem CID: 2264
  ChEBI ID: CHEBI:91712
  CAS Number: CAS 123040-69-7
  TTD Drug ID: DMDPM7R
  VARIDT Drug ID: DR01499

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 3 receptor (5HT3R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ondansetron	DMOTQ1I	Chemotherapy-induced nausea	MD90	Approved	[4]
Granisetron	DMIUW25	Malignant glioma	2A00.0	Approved	[5]
Ramosetron	DMH7GN8	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[6]
Renzapride	DM7HQNX	Irritable bowel syndrome	DD91.0	Phase 3	[7]
LITOXETINE	DMKZRBP	Mood disorder	6A60-6E23	Phase 3	[8]
Zatosetron maleate	DMWDEFC	Anxiety disorder	6B00-6B0Z	Phase 3	[9]
Pancopride	DMIRYU9	Nausea	MD90	Phase 3	[10]
Lerisetron	DMOTCIU	Nausea	MD90	Phase 3	[11]
Lintopride	DMSHGWN	Nausea	MD90	Phase 2	[12]
DDP-225	DM9REBL	Irritable bowel syndrome	DD91.0	Phase 2	[13]

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	[3]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[14]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[15]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[16]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[15]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[15]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[17]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[15]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[18]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 3 receptor (5HT3R)	TTNXLKE	NOUNIPROTAC	Antagonist	[2]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[3]

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: 2285).
• [2] The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist. Eur J Pharmacol. 1991 Apr 24;196(3):299-305.
• [3] Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
• [4] Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron: a randomized, placebo-controlled, double-blind cross-over trial. Eur J Gastroenterol Hepatol. 1998 Oct;10(10):865-70.
• [5] New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7.
• [6] Inhibitory effect of YM060 on 5-HT3 receptor-mediated depolarization in colonic myenteric neurons of the guinea pig. Eur J Pharmacol. 1995 Sep 5;283(1-3):107-12.
• [7] Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63.
• [8] Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45.
• [9] Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety. J Clin Psychopharmacol. 1999 Apr;19(2):125-31.
• [10] Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol. 1992 Nov 10;222(2-3):257-64.
• [11] Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
• [12] The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
• [13] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [14] MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
• [15] 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.
• [16] Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
• [17] Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
• [18] Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
• [19] 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.