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

General Information of Drug (ID: DM0X36Y)

• Drug Name: Ritanserin Drug Info
• Synonyms: ritanserin; 87051-43-2; Tiserton; Ritanserine; Ritanserinum; Ritanserina; R-55667; Ritanserinum [Latin]; Ritanserine [French]; Ritanserina [Spanish]; UNII-145TFV465S; C27H25F2N3OS; R 55,667; 6-(2-(4-(bis(4-fluorophenyl)methylene)piperidin-1-yl)ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one; MLS000069360; CHEMBL267777; 6-(2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-7-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one; N,N-dialkyl-dipeptidylamines

Indication

Disease Entry	ICD 11	Status	REF
Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 5074
  ChEBI ID: CHEBI:64195
  CAS Number: CAS 87051-43-2
  TTD Drug ID: DM0X36Y

Molecule-Related Drug Atlas

Drug(s) Targeting 5-HT 2B receptor (HTR2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[7]
Triflupromazine	DMKFQJP	Nausea	MD90	Approved	[8]
Minaprine	DM0EP7M	Depression	6A70-6A7Z	Approved	[9]
SPN-812	DMTV7XH	Attention deficit hyperactivity disorder	6A05.Z	Phase 4	[10]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[11]
PRX-08066	DMR7H2V	Pulmonary arterial hypertension	BB01.0	Phase 2	[12]
Pyrimidine derivative 29	DMVOYJ8	N. A.	N. A.	Patented	[13]
Pyrimidine derivative 26	DM90WKN	N. A.	N. A.	Patented	[13]
Pyrimidine derivative 23	DM5MLQU	N. A.	N. A.	Patented	[13]
Pyrimidine derivative 25	DM51MFS	N. A.	N. A.	Patented	[13]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[7]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[14]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[15]
Flibanserin	DM70DTN	Depression	6A70-6A7Z	Approved	[16]
Lurasidone hydrochloride	DMCVPXO	Schizophrenia	6A20	Approved	[17]
Aniracetam	DMOIFW0	Cerebrovascular ischaemia	8B1Z	Approved	[18]
lumateperone tosylate	DMQ8HOJ	Schizophrenia	6A20	Approved	[19]
Sarpogrelate	DMGLP6S	Diabetic complication	5A2Y	Approved	[20]
Pimavanserin	DMR7IVC	Parkinson disease	8A00.0	Approved	[21]
Zicronapine	DMP8ESD	Schizophrenia	6A20	Phase 3	[22]

Drug(s) Targeting Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LOMERIZINE	DME0TC8	Migraine	8A80	Approved	[23]
Ziconotide	DMSLJP4	Pain	MG30-MG3Z	Approved	[24]
Hesperidin	DMI5DW1	Vascular purpura	3B60	Approved	[25]
Cilnidipine	DM1975O	High blood pressure	BA00	Phase 3	[26]
Ralfinamide	DMUNMY0	Neuropathic pain	8E43.0	Phase 3	[27]
CNV-2197944	DMLT7JV	Pain	MG30-MG3Z	Phase 2	[28]
CNSB-004	DMHAI0M	Pain	MG30-MG3Z	Preclinical	[29]
TH-9229	DMG1MPD	Reperfusion injury	ND56.Z	Terminated	[30]
PD-157667	DM61NFD	N. A.	N. A.	Terminated	[31]
PD-0204318	DMGKVPH	Pain	MG30-MG3Z	Terminated	[32]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mianserin	DMVKA4O	Depression	6A70-6A7Z	Approved	[33]
Cyclobenzaprine	DM1YBRM	Depression	6A70-6A7Z	Approved	[34]
Perospirone	DMVHJLX	Psychotic disorder	6A20-6A25	Approved	[35]
Ketanserin	DMVLMW6	Hypertension	BA00-BA04	Approved	[36]
Bis(olanzapine) pamoate monohydrate	DME76AP	Psychotic disorder	6A20-6A25	Phase 3	[37]
FKB01MD	DM2O7NM	N. A.	N. A.	Phase 2	[38]
Nexopamil	DML5S71	Hypertension	BA00-BA04	Phase 2	[39]
TGWOOAA	DMI57ZA	Generalized anxiety disorder	6B00	Phase 2	[40]
TGOF02N	DMQ6ANE	Schizophrenia	6A20	Phase 2	[41]
AMAP-102	DM7CD8Z	Arthritis	FA20	Phase 1	[42]

Drug(s) Targeting 5-HT 2C receptor (HTR2C)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[7]
Lorcaserin	DMG6OYJ	Obesity	5B81	Approved	[43]
Tramadol	DMRQD04	Osteoarthritis	FA00-FA05	Approved	[44]
Mirtazapine	DML53ZJ	Depression	6A70-6A7Z	Approved	[45]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[46]
Methysergide	DM1EF73	Migraine	8A80	Approved	[47]
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[48]
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[49]
SR46349B	DM1ODMR	Primary insomnia	7A00	Phase 3	[50]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[11]

Drug(s) Targeting 5-HT receptor (5HTR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[51]
Paliperidone	DM7NPJS	Psychotic disorder	6A20-6A25	Approved	[37]
Ramosetron	DMH7GN8	Diarrhea-predominant irritable bowel syndrome	DD91.01	Approved	[51]
Pizotyline	DMV74ZH	Headache	8A80-8A84	Approved	[37]
Tandospirone	DMPHWU6	Anxiety disorder	6B00-6B0Z	Approved	[51]
Nafronyl	DMVMQ1L	Cerebrovascular ischaemia	8B1Z	Approved	[37]
ITI-007	DMUQ1DO	Depression	6A70-6A7Z	Phase 3	[38]
Fenfluramine	DM0762O	Dravet syndrome	8A61.11	Phase 3	[52]
MIN-117	DMSLIW6	Major depressive disorder	6A70.3	Phase 2	[38]
Lu-AA34893	DM2ZUXK	Anxiety disorder	6B00-6B0Z	Phase 2	[53]

Drug(s) Affected By Transcription factor SOX-17 (SOX17)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[6]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[6]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[6]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[6]
Thalidomide	DM70BU5	Adult T-cell leukemia/lymphoma		Approved	[6]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[6]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[54]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[55]
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[6]
Ziprasidone	DMM58JY	Bipolar disorder	6A60	Approved	[6]

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]
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Antagonist	[2]
5-HT 2B receptor (HTR2B)	TT0K1SC	5HT2B_HUMAN	Antagonist	[3]
5-HT 2C receptor (HTR2C)	TTWJBZ5	5HT2C_HUMAN	Antagonist	[2]
5-HT receptor (5HTR)	TT85JO3	NOUNIPROTAC	Antagonist	[4]
Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)	TT4FDG6	CAC1B_HUMAN	Blocker	[5]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Transcription factor SOX-17 (SOX17)	OT9H4WWE	SOX17_HUMAN	Protein Interaction/Cellular Processes	[6]

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: 97).
• [2] Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7.
• [3] p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.
• [4] Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82.
• [5] N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12.
• [6] A high-throughput screen for teratogens using human pluripotent stem cells. Toxicol Sci. 2014 Jan;137(1):76-90. doi: 10.1093/toxsci/kft239. Epub 2013 Oct 23.
• [7] 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.
• [8] Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
• [9] Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
• [10] New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
• [11] Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
• [12] Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
• [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] Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
• [15] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [16] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [17] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [18] 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.
• [19] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [20] 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.
• [21] 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.
• [22] Clinical pipeline report, company report or official report of Lundbeck.
• [23] Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7.
• [24] Emerging treatments for traumatic brain injury. Expert Opin Emerg Drugs. 2009 Mar;14(1):67-84.
• [25] In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
• [26] N- and L-type calcium channel antagonist improves glomerular dynamics, reverses severe nephrosclerosis, and inhibits apoptosis and proliferation in an l-NAME/SHR model. J Hypertens. 2002 May;20(5):993-1000.
• [27] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [28] Clinical pipeline report, company report or official report of Convergence Pharmaceuticals Ltd.
• [29] CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain. Pain Med. 2010 Feb;11(2):262-73.
• [30] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008159)
• [31] Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.
• [32] US patent application no. 2012,0172,429, Permanently charged sodium and calcium channel blockers as anti- inflammatory agents.
• [33] 5-HT reuptake and 5-HT2 receptors modulate capsaicin-evoked hypothermia in rats. Neurosci Lett. 2008 Jan 17;430(3):191-6.
• [34] Torticollis under Cyclobenzaprine. Pharmacology. 2009 Jul 8;84(2):91-92.
• [35] Pharmacological effects of zotepine and other antipsychotics on the central 5-HT2 receptors. Pharmacopsychiatry. 1993 Mar;26(2):53-8.
• [36] Nordexfenfluramine causes more severe pulmonary vasoconstriction than dexfenfluramine. Am J Physiol Lung Cell Mol Physiol. 2004 Mar;286(3):L531-8.
• [37] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [38] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [39] 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.
• [40] Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
• [41] Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
• [42] Clinical pipeline report, company report or official report of Anamar.
• [43] Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
• [44] The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
• [45] Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulatio... Mol Pharmacol. 2008 Mar;73(3):748-57.
• [46] Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60.
• [47] Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8.
• [48] Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
• [49] Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
• [50] SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 2002 Sep;27(3):430-41.
• [51] Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
• [52] Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.
• [53] Encyclopedia of Psychopharmacology. Ian Stolerman. 2010. Page(105).
• [54] Antiepileptic drugs are endocrine disruptors for the human fetal testis ex vivo. Toxicol Sci. 2023 Sep 28;195(2):169-183. doi: 10.1093/toxsci/kfad076.
• [55] Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.