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

General Information of Drug (ID: DMVLMW6)

• Drug Name: Ketanserin Drug Info
• Synonyms: Ketanserina; Ketanserine; Ketanserinum; Ketaserin; Perketal; Serefrex; Sufrexal; Taseron; Ketanserina [INN-Spanish]; Ketanserine [INN-French]; Ketanserinum [INN-Latin]; R 41,468; R-41468; [3H]-Ketanserin; Ketanserin (USAN/INN); Ketanserin [USAN:BAN:INN]; R-41,468; (+)-3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4(1H,3H)-quinazolinedione; 3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione; 3-(2-(4-(p-Fluorobenzoyl)piperidino)ethyl)-2,4-(1H,3H)-quinazolinedione; 3-(2-{4-[(4-fluorophenyl)carbonyl]piperidin-1-yl}ethyl)quinazoline-2,4(1H,3H)-dione; 3-[2-[4-(4-fluorobenzoyl)-1-piperidyl]ethyl]-1H-quinazoline-2,4-dione; 3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione; 3-{2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl}quinazoline-2,4(1H,3H)-dione

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Approved	[1]

• Therapeutic Class: Antihypertensive Agents
• Cross-matching ID:
  PubChem CID: 3822
  ChEBI ID: CHEBI:6123
  CAS Number: CAS 74050-98-9
  TTD Drug ID: DMVLMW6

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 2 receptor (5HT2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mianserin	DMVKA4O	Depression	6A70-6A7Z	Approved	[4]
Cyclobenzaprine	DM1YBRM	Depression	6A70-6A7Z	Approved	[5]
Perospirone	DMVHJLX	Psychotic disorder	6A20-6A25	Approved	[6]
Bis(olanzapine) pamoate monohydrate	DME76AP	Psychotic disorder	6A20-6A25	Phase 3	[7]
FKB01MD	DM2O7NM	N. A.	N. A.	Phase 2	[8]
Nexopamil	DML5S71	Hypertension	BA00-BA04	Phase 2	[9]
TGWOOAA	DMI57ZA	Generalized anxiety disorder	6B00	Phase 2	[10]
TGOF02N	DMQ6ANE	Schizophrenia	6A20	Phase 2	[11]
AMAP-102	DM7CD8Z	Arthritis	FA20	Phase 1	[12]
Heterocyclic-tetracyclic tetrahydrofuran derivative 1	DMNJVR6	N. A.	N. A.	Patented	[13]

Drug(s) Affected By 5-hydroxytryptamine receptor 2A (HTR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gabapentin	DM6T924	Complex partial seizure	8A68.0	Approved	[14]
Fluphenazine	DMIT8LX	Psychotic disorder	6A20-6A25	Approved	[15]
Paliperidone	DM7NPJS	Psychotic disorder	6A20-6A25	Approved	[16]
Haloperidol	DM96SE0	Delirium		Approved	[16]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[17]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[18]
Olanzapine	DMPFN6Y	Bipolar depression		Approved	[19]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[20]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[21]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2 receptor (5HT2R)	TTYSN63	NOUNIPROTAC	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
5-hydroxytryptamine receptor 2A (HTR2A)	OTWXJX0M	5HT2A_HUMAN	Gene/Protein Processing	[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: 88).
• [2] Nordexfenfluramine causes more severe pulmonary vasoconstriction than dexfenfluramine. Am J Physiol Lung Cell Mol Physiol. 2004 Mar;286(3):L531-8.
• [3] The role of MAPK and Nrf2 pathways in ketanserin-elicited attenuation of cigarette smoke-induced IL-8 production in human bronchial epithelial cells. Toxicol Sci. 2012 Feb;125(2):569-77. doi: 10.1093/toxsci/kfr305. Epub 2011 Nov 1.
• [4] 5-HT reuptake and 5-HT2 receptors modulate capsaicin-evoked hypothermia in rats. Neurosci Lett. 2008 Jan 17;430(3):191-6.
• [5] Torticollis under Cyclobenzaprine. Pharmacology. 2009 Jul 8;84(2):91-92.
• [6] Pharmacological effects of zotepine and other antipsychotics on the central 5-HT2 receptors. Pharmacopsychiatry. 1993 Mar;26(2):53-8.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] Inhibition by the combined Ca2+ and 5-HT2 receptor antagonist nexopamil (LU 49938) of intracoronary thrombus formation in a canine model of arterial stenosis and intimal damage. J Cardiovasc Pharmacol. 1993 Nov;22(5):687-94.
• [10] Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
• [11] Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
• [12] Clinical pipeline report, company report or official report of Anamar.
• [13] Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
• [14] 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.
• [15] Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. doi: 10.1073/pnas.0609752104. Epub 2007 Jul 2.
• [16] Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12.
• [17] 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.
• [18] Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
• [19] No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. doi: 10.1038/sj.tpj.6500418. Epub 2006 Sep 19.
• [20] Nephrotoxicity induced by cisplatin is primarily due to the activation of the 5-hydroxytryptamine degradation system in proximal renal tubules. Chem Biol Interact. 2021 Nov 1;349:109662. doi: 10.1016/j.cbi.2021.109662. Epub 2021 Sep 21.
• [21] Prenatal arsenic exposure and the epigenome: identifying sites of 5-methylcytosine alterations that predict functional changes in gene expression in newborn cord blood and subsequent birth outcomes. Toxicol Sci. 2015 Jan;143(1):97-106. doi: 10.1093/toxsci/kfu210. Epub 2014 Oct 10.
• [22] Endometrial receptivity is affected in women with high circulating progesterone levels at the end of the follicular phase: a functional genomics analysis. Hum Reprod. 2011 Jul;26(7):1813-25.