General Information of Drug (ID: DMQ0IOF)

Drug Name
ICI-169369 Drug Info
Synonyms
2-Detpq; Ici 169369; 2-((2-(dimethylamino)ethyl)thio)-3-phenylquinoline; 85273-95-6; Ici-169,369; UNII-4CT4CS5BA7; ICI-169369; 4CT4CS5BA7; N,N-dimethyl-2-(3-phenylquinolin-2-yl)sulfanylethanamine; Ethanamine, N,N-dimethyl-2-((3-phenyl-2-quinolinyl)thio)-; Ethanamine, N,N-dimethyl-2-[(3-phenyl-2-quinolinyl)thio]-; AC1L3UA4; GTPL273; AC1Q7E25; SCHEMBL2640021; CHEMBL1191534; CTK2I4265; BDBM84945; DTXSID40234468; 85273-96-7 (hydrochloride); n,n-dimethyl-2-[(3-phenylquinolin-2-yl)sulfanyl]ethanamine; ZINC5140456; PDSP2_001405
Indication
Disease Entry ICD 11 Status REF
Anxiety disorder 6B00-6B0Z Terminated [1]
Cross-matching ID
PubChem CID
122265
CAS Number
CAS 85273-95-6
TTD Drug ID
DMQ0IOF

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
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]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2C receptor (HTR2C)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [4]
Lorcaserin DMG6OYJ Obesity 5B81 Approved [14]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [15]
Mirtazapine DML53ZJ Depression 6A70-6A7Z Approved [16]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [17]
Methysergide DM1EF73 Migraine 8A80 Approved [18]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [19]
M100907 DM7ZFBA Sleep-wake disorder 7A00-7B2Z Phase 3 [20]
SR46349B DM1ODMR Primary insomnia 7A00 Phase 3 [21]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [22]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [23]
Cyproheptadine DM92AH3 Allergic rhinitis CA08.0 Approved [3]
Clozapine DMFC71L Schizophrenia 6A20 Approved [3]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [24]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [25]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [26]
PD-0325901 DM27D4J Breast cancer 2C60-2C65 Phase 2 [27]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [28]
SL65.0472 DMU5RKC Cardiovascular disease BA00-BE2Z Discontinued in Phase 2 [29]
SB-269970 DM8WTGA Sleep-wake disorder 7A00-7B2Z Terminated [3]
⏷ 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 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Modulator [2]
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Modulator [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
5-hydroxytryptamine receptor 7 (HTR7) OT44DEWB 5HT7R_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: 273).
2 Serotonin 5-HT(2A) receptor antagonists in the treatment of insomnia: present status and future prospects.Drugs Today (Barc).2010 Mar;46(3):183-93.
3 Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions. Psychopharmacology (Berl). 2010 Dec;212(4):687-97. doi: 10.1007/s00213-010-2001-x. Epub 2010 Sep 9.
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 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
15 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.
16 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.
17 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.
18 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.
19 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
20 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.
21 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.
22 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.
23 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
24 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
25 Multi-level gene expression profiles affected by thymidylate synthase and 5-fluorouracil in colon cancer. BMC Genomics. 2006 Apr 3;7:68. doi: 10.1186/1471-2164-7-68.
26 Physiogenomic association of statin-related myalgia to serotonin receptors. Muscle Nerve. 2007 Sep;36(3):329-35. doi: 10.1002/mus.20871.
27 PRC2 loss amplifies Ras-driven transcription and confers sensitivity to BRD4-based therapies. Nature. 2014 Oct 9;514(7521):247-51.
28 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
29 Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95.