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

General Information of Drug (ID: DMFU9VH)

• Drug Name: GR-113808 Drug Info
• Synonyms: CHEMBL518682; GTPL259; [3H]GR 113808; GR 125487 [H3]; [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-(tritritiomethyl)indole-3-carboxylate

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 119376
  ChEBI ID: CHEBI:73380
  CAS Number: CAS 144625-51-4
  TTD Drug ID: DMFU9VH

Molecule-Related Drug Atlas

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]

Drug(s) Affected By 5-hydroxytryptamine receptor 4 (HTR4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selenium	DM25CGV	N. A.	N. A.	Approved	[13]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[14]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[15]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[16]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[17]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 4 receptor (HTR4)	TT07C3Y	5HT4R_HUMAN	Inhibitor	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
5-hydroxytryptamine receptor 4 (HTR4)	OTBIB44K	5HT4R_HUMAN	Protein Interaction/Cellular Processes	[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: 259).
• [2] Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers. J Med Chem. 2007 Sep 6;50(18):4482-92.
• [3] New arylpiperazine derivatives as antagonists of the human cloned 5-HT(4) receptor isoforms. J Med Chem. 2000 Oct 5;43(20):3761-9. doi: 10.1021/jm0009538.
• [4] Metoclopramide stimulates catecholamine- and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5... Endocr Relat Cancer. 2009 Mar;16(1):281-90.
• [5] Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
• [6] Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
• [7] 5-Hydroxytryptamine mediated contractions in isolated preparations of equine ileum and pelvic flexure: pharmacological characterization of a new 5-HT(4) agonist. J Vet Pharmacol Ther. 2002 Feb;25(1):49-58.
• [8] The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.
• [9] 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.
• [10] The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
• [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] 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.
• [14] The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
• [15] 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.
• [16] The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
• [17] Gene expression profiling of 30 cancer cell lines predicts resistance towards 11 anticancer drugs at clinically achieved concentrations. Int J Cancer. 2006 Apr 1;118(7):1699-712. doi: 10.1002/ijc.21570.
• [18] 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.