General Information of Drug (ID: DMB9VGW)

Drug Name
[3H]granisetron Drug Info
Synonyms [3H]-granisetron; [3H]-BRL-43694
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
3510
CAS Number
CAS 109889-09-0
TTD Drug ID
DMB9VGW

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting 5-HT 3B receptor (HTR3B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [4]
SEROTONIN DMOFCRY Discovery agent N.A. Investigative [5]
2-methyl-5-HT DM1S5CB N. A. N. A. Investigative [6]
QUIPAZINE DMPY6IG Discovery agent N.A. Investigative [5]
MESULERGINE DMKGWAH Discovery agent N.A. Investigative [7]
bilobalide DM09Z35 Discovery agent N.A. Investigative [8]
2-(4-Methyl-piperazin-1-yl)-quinoline DMB8OY6 Discovery agent N.A. Investigative [5]
BRL-24682 DMSB4EW Discovery agent N.A. Investigative [9]
6-(4-Methyl-piperazin-1-yl)-phenanthridine DM1HAWR Discovery agent N.A. Investigative [5]
trichloroethanol DMNALMF Discovery agent N.A. Investigative [10]
⏷ 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 [11]
Alosetron DML2A03 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [12]
Tropisetron DMNSJ7V Fibromyalgia MG30.01 Approved [13]
Palonosetron DMBHMOX Nausea MD90 Approved [14]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [13]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [15]
Cilansetron DMP0NGX Irritable bowel syndrome DD91.0 Phase 3 [16]
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [4]
Norcisapride DMJSKUI Gastroesophageal reflux disease DA22.Z Discontinued in Phase 2 [17]
YM-114 DML2IXO Nausea MD90 Discontinued in Phase 2 [18]
⏷ 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
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Antagonist [2]
5-HT 3B receptor (HTR3B) TTR6K75 5HT3B_HUMAN Antagonist [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: 2292).
2 Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells. Br J Pharmacol. 1996 Jul;118(5):1237-45.
3 Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors. Neuropharmacology. 2001 Aug;41(2):282-4.
4 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.
5 Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy ... J Med Chem. 1999 May 6;42(9):1556-75.
6 The 5-HT3B subunit is a major determinant of serotonin-receptor function. Nature. 1999 Jan 28;397(6717):359-63.
7 Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. J Med Chem. 1997 Oct 24;40(22):3670-8.
8 Ginkgolide B and bilobalide block the pore of the 5-HT eceptor at a location that overlaps the picrotoxin binding site. Neuropharmacology. 2011 Feb-Mar;60(2-3):488-95.
9 Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotoni... J Med Chem. 2003 Feb 27;46(5):702-15.
10 Co-expression of the 5-HT(3B) subunit with the 5-HT(3A) receptor reduces alcohol sensitivity. Brain Res Mol Brain Res. 2005 Dec 14;142(2):146-50.
11 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.
12 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.
13 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
14 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
15 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.
16 Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
17 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.
18 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.