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

General Information of Drug (ID: DMMHSYA)

• Drug Name: [3H]GR65630 Drug Info
• Synonyms: [3H]-GR65630

Indication

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

• Cross-matching ID:
  PubChem CID: 5311136
  ChEBI ID: CHEBI:87784
  TTD Drug ID: DMMHSYA

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 3A receptor (HTR3A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dolasetron	DMMG26Z	Nausea	MD90	Approved	[4]
Alosetron	DML2A03	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[5]
Tropisetron	DMNSJ7V	Fibromyalgia	MG30.01	Approved	[6]
Palonosetron	DMBHMOX	Nausea	MD90	Approved	[7]
Levetiracetam	DMTGDN8	Epilepsy	8A60-8A68	Approved	[6]
Procaine	DM4LSNE	Anaesthesia	9A78.6	Approved	[8]
Cilansetron	DMP0NGX	Irritable bowel syndrome	DD91.0	Phase 3	[9]
BEMESETRON	DMSPJX9	N. A.	N. A.	Discontinued in Phase 3	[10]
Norcisapride	DMJSKUI	Gastroesophageal reflux disease	DA22.Z	Discontinued in Phase 2	[11]
YM-114	DML2IXO	Nausea	MD90	Discontinued in Phase 2	[12]

Drug(s) Affected By 5-hydroxytryptamine receptor 3A (HTR3A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gabapentin	DM6T924	Complex partial seizure	8A68.0	Approved	[13]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[14]
Methylprednisolone	DM4BDON	Acute adrenal insufficiency		Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[3]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[17]
Hydromorphone	DMHP21E	Back pain	ME84.Z	Approved	[18]
Rosiglitazone	DMILWZR	Chronic kidney disease	GB61	Approved	[19]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[15]
Decitabine	DMQL8XJ	Acute myelogenous leukaemia	2A41	Approved	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 3A receptor (HTR3A)	TTPC4TU	5HT3A_HUMAN	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
5-hydroxytryptamine receptor 3A (HTR3A)	OTAIV1AK	5HT3A_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: 2303).
• [2] Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome. J Pharmacol Sci. 2007 Jul;104(3):263-73.
• [3] Interactions of metoclopramide and ergotamine with human 5-HT(3A) receptors and human 5-HT reuptake carriers. Br J Pharmacol. 2005 Oct;146(4):543-52. doi: 10.1038/sj.bjp.0706351.
• [4] 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.
• [5] Efficacy of 5-HT3 antagonists and 5-HT4 agonists in irritable bowel syndrome: systematic review and meta-analysis. Am J Gastroenterol. 2009 Jul;104(7):1831-43; quiz 1844.
• [6] Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
• [7] Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
• [8] Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors. Reg Anesth Pain Med. 2007 Nov-Dec;32(6):462-70.
• [9] Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
• [10] Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9.
• [11] mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83.
• [12] Effect of serotonin (5-HT)3-receptor antagonists YM060, YM114 (KAE-393), ondansetron and granisetron on 5-HT4 receptors and gastric emptying in rodents. Jpn J Pharmacol. 1995 Nov;69(3):205-14.
• [13] 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.
• [14] Acute hypersensitivity of pluripotent testicular cancer-derived embryonal carcinoma to low-dose 5-aza deoxycytidine is associated with global DNA Damage-associated p53 activation, anti-pluripotency and DNA demethylation. PLoS One. 2012;7(12):e53003. doi: 10.1371/journal.pone.0053003. Epub 2012 Dec 27.
• [15] Inhibitory effect of glucocorticoids on human-cloned 5-hydroxytryptamine3A receptor expressed in xenopus oocytes. Anesthesiology. 2004 Sep;101(3):660-5. doi: 10.1097/00000542-200409000-00014.
• [16] Design principles of concentration-dependent transcriptome deviations in drug-exposed differentiating stem cells. Chem Res Toxicol. 2014 Mar 17;27(3):408-20.
• [17] Activation and modulation of recombinantly expressed serotonin receptor type 3A by terpenes and pungent substances. Biochem Biophys Res Commun. 2015 Nov 27;467(4):1090-6. doi: 10.1016/j.bbrc.2015.09.074. Epub 2015 Oct 9.
• [18] The effects of fentanyl-like opioids and hydromorphone on human 5-HT3A receptors. Anesth Analg. 2008 Jul;107(1):107-12. doi: 10.1213/ane.0b013e31817342c2.
• [19] 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.