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

General Information of Drug (ID: DME694O)

• Drug Name: Fananserin Drug Info
• Synonyms: 127625-29-0; RP 62203; Fananserin [USAN:INN]; RP-62203; UNII-38QJ762ET6; CHEMBL83894; C23H24FN3O2S; VGIGHGMPMUCLIQ-UHFFFAOYSA-N; 38QJ762ET6; NCGC00167808-01; DSSTox_RID_81871; DSSTox_CID_26743; 2-(3-(4-(p-Fluorophenyl)-1-piperazinyl)propyl)-2H-naphth(1,8-cd)isothiazole 1,1-dioxide; 2H-Naphth(1,8-cd)isothiazole, 2-(3-(4-(4-fluorophenyl)-1-piperazinyl)propyl)-, 1,1-dioxide; DSSTox_GSID_46743; [3H]fananserin; CAS-127625-29-0; Fananserin (USAN/INN); [3H]RP62203; [3H]RP-62203; AC1L1TX5; RP 62203; 2-(3-(4-(4-fluorophenyl)-1-piperazinyl)propyl)-2H-naphth(1,8-cd)isothiazole 1,1-dioxide

Indication

Disease Entry	ICD 11	Status	REF
Schizophrenia	6A20	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 60785
  ChEBI ID: CHEBI:92159
  CAS Number: CAS 127625-29-0
  TTD Drug ID: DME694O
  VARIDT Drug ID: DR00789

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 2A receptor (HTR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[4]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[5]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[6]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[7]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[8]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[9]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[10]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[11]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[12]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[13]

Drug(s) Affected By Potassium voltage-gated channel subfamily H member 2 (KCNH2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metoclopramide	DMFA5MY	Nausea	MD90	Approved	[14]
Quinidine	DMLPICK	N. A.	N. A.	Approved	[15]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[16]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[17]
Clarithromycin	DM4M1SG	Acute maxillary sinusitis		Approved	[17]
Disopyramide	DM5SYZP	Long QT syndrome	BC65.0	Approved	[18]
Propranolol	DM79NTF	Angina pectoris	BA40	Approved	[19]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[20]
Dofetilide	DMPN1TW	Sinus rhythm disorder	BC9Y	Approved	[21]
Flecainide	DMSQDLE	Tachyarrhythmias	BC71	Approved	[17]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Antagonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Potassium voltage-gated channel subfamily H member 2 (KCNH2)	OTZX881H	KCNH2_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: 5434).
• [2] Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. Pharmacological characterization of [3H]RP 62203 binding in the rat brain. Eur J Pharmacol. 1993 Mar 16;233(1):37-45.
• [3] Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
• [4] Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
• [5] Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
• [6] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [7] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [8] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [9] Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.
• [10] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [11] Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
• [12] Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
• [13] Clinical pipeline report, company report or official report of Lundbeck.
• [14] Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
• [15] Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
• [16] Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
• [17] Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
• [18] Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
• [19] Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
• [20] Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
• [21] Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.