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

General Information of Drug (ID: DM0UADK)

Drug Name
OCTOCLOTHEPIN Drug Info
Synonyms
Clorotepine; Octoclothepin; Octoclothepine; Clotepin; Clothepin; 13448-22-1; Clorotepine [INN]; Clorotepinum [INN-Latin]; Clorotepina [INN-Spanish]; CHEMBL64249; 1-(8-Chloro-10,11-dihydrodibenzo(b,f)thiepin-10-yl)-4-methylpiperazine; Piperazine, 1-(8-chloro-10,11-dihydrodibenzo(b,f)thiepin-10-yl)-4-methyl-; clothepine; clorothepin; Clorotepinum; Clorotepina; 1-(8-chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine; VUFB-6281; Octoclothepin maleate; CLOROTEPINE(-); AC1Q3SXZ; CLOROTEPINE (+); OCTOCLOTHEPIN,(-)
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
1238
ChEBI ID
CHEBI:135459
CAS Number
CAS 13448-22-1
TTD Drug ID
DM0UADK

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Approved Drug(s)
Discontinued Drug(s)
Patented Agent(s)
Download the Complete Related Drug List
Drug(s) Targeting 5-HT 6 receptor (HTR6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LU AE58054 DMWGRQD Schizophrenia 6A20 Phase 3 [4]
SB-742457 DM6L4ZT Alzheimer disease 8A20 Phase 3 [5]
AVN 211 DMVB4OS Schizophrenia 6A20 Phase 2/3 [6]
SYN120 DMDF7XB Parkinson disease 8A00.0 Phase 2 [7]
AVN 101 DMJFLBC Alzheimer disease 8A20 Phase 2 [6]
SYN-120 DMPW0UL Alzheimer disease 8A20 Phase 2 [8]
PF-05212377 DMPVQYR Alzheimer disease 8A20 Phase 2 [9]
AVN 322 DMK2LGM Cognitive impairment 6D71 Phase 2 [5]
SAM-531 DMHVJZ6 Alzheimer disease 8A20 Phase 2 [10]
SUVN-502 DMQD753 Alzheimer disease 8A20 Phase 2 [11]
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Drug(s) Targeting Adrenergic receptor alpha-1B (ADRA1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methamphetamine DMPM4SK Anxiety Approved [12]
Propericiazine DME9JNL Psychiatric disorder 6E8Z Approved [13]
Methoxamine DMF5XQH Hypertension BA00-BA04 Approved [14]
Phendimetrazine DM6TS1N Obesity 5B81 Approved [15]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [16]
TIOSPIRONE DME5QDP N. A. N. A. Discontinued in Phase 3 [17]
Sunepitron DM6M8ZX N. A. N. A. Discontinued in Phase 3 [18]
MAZAPERTINE DMRHYAU N. A. N. A. Discontinued in Phase 2 [19]
SOU-001 DMPAEK5 Urinary incontinence MF50.2 Discontinued in Phase 2 [20]
SNAP-5089 DMROJEN Heart arrhythmia BC65 Terminated [21]
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Drug(s) Targeting Adrenergic receptor alpha-1D (ADRA1D)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxazosin DM9PLRH Benign prostatic hyperplasia GA90 Approved [22]
Armodafinil DMGB035 Malignant glioma 2A00.0 Approved [23]
Alfuzosin DMZVMKF Benign prostatic hyperplasia GA90 Approved [24]
Moxisylyte DMFCLYW Erectile dysfunction HA01.1 Approved [25]
Terazosin DM3JCVS Benign prostatic hyperplasia GA90 Approved [26]
Bunazosin DM4I8O7 Glaucoma/ocular hypertension 9C61 Approved [27]
Trimazosin DM1QLST Congestive heart failure BD10 Approved [28]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [16]
DL-017 DMM8GZT Hypertension BA00-BA04 Phase 1 [29]
PMID30124346-Compound-LDT8 DM5MUNG Benign prostatic hyperplasia GA90 Patented [30]
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Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [31]
Haloperidol DM96SE0 Delirium Approved [32]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [33]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [34]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [35]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [36]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [37]
Pimozide DMW83TP Schizophrenia 6A20 Approved [38]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [39]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [40]
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Drug(s) Targeting Histamine H1 receptor (H1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [41]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [42]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [43]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [44]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [45]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [43]
Doxepin DMPI98T Anxiety Approved [46]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [43]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [47]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [48]
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Drug(s) Targeting 5-HT 2C receptor (HTR2C)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [49]
Lorcaserin DMG6OYJ Obesity 5B81 Approved [50]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [51]
Mirtazapine DML53ZJ Depression 6A70-6A7Z Approved [52]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [53]
Methysergide DM1EF73 Migraine 8A80 Approved [54]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [55]
M100907 DM7ZFBA Sleep-wake disorder 7A00-7B2Z Phase 3 [56]
SR46349B DM1ODMR Primary insomnia 7A00 Phase 3 [57]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [58]
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Drug(s) Targeting Adrenergic receptor alpha-1A (ADRA1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
SILODOSIN DMJSBT6 Benign prostatic hyperplasia GA90 Approved [59]
NAFTOPIDIL DMQ8R4E Hypertension BA00-BA04 Approved [59]
Tamsulosin DM5QF9V Benign prostatic hyperplasia GA90 Approved [60]
Xatral DMLHOA0 Benign prostatic hyperplasia GA90 Approved [61]
Dutasteride + tamsulosin DM6P8HU Benign prostatic hyperplasia GA90 Phase 3 [62]
Besipirdine DMLVNTA Cognitive impairment 6D71 Phase 3 [63]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [16]
PMID30124346-Compound-LDT8 DM5MUNG Benign prostatic hyperplasia GA90 Patented [30]
PMID30124346-Compound-LDT66 DMJMTNL Benign prostatic hyperplasia GA90 Patented [30]
TIOSPIRONE DME5QDP N. A. N. A. Discontinued in Phase 3 [17]
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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 [64]
Quinidine DMLPICK N. A. N. A. Approved [65]
Verapamil DMA7PEW Angina pectoris BA40 Approved [66]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [67]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [67]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [68]
Propranolol DM79NTF Angina pectoris BA40 Approved [69]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [70]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [71]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [67]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Inhibitor [1]
5-HT 6 receptor (HTR6) TTJS8PY 5HT6R_HUMAN Inhibitor [2]
Adrenergic receptor alpha-1A (ADRA1A) TTNGILX ADA1A_HUMAN Inhibitor [1]
Adrenergic receptor alpha-1B (ADRA1B) TTBRKXS ADA1B_HUMAN Inhibitor [1]
Adrenergic receptor alpha-1D (ADRA1D) TT34BHT ADA1D_HUMAN Inhibitor [1]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Inhibitor [1]
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Inhibitor [1]

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 Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adre... J Med Chem. 2010 Oct 14;53(19):7021-34.
2 Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J Med Chem. 2005 Mar 24;48(6):1781-95.
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 Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.
5 5-HT6 receptors and Alzheimer's disease. Alzheimers Res Ther. 2013; 5(2): 15.
6 Latrepirdine, a potential novel treatment for Alzheimer's disease and Huntington's chorea. Curr Opin Investig Drugs. 2010 January; 11(1): 80-91.
7 Therapeutic strategies for Parkinson disease: beyond dopaminergic drugs. Nat Rev Drug Discov. 2018 Nov;17(11):804-822.
8 The Serotonin-6 Receptor as a Novel Therapeutic Target. Exp Neurobiol. 2011 December; 20(4): 159-168.
9 PF-05212377 Alzheimer's Disease (Phase 2). Pfizer.
10 Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9.
11 Novel and Potent 5-Piperazinyl Methyl-N1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands. ACS Med Chem Lett. 2010 October 14; 1(7): 340-344.
12 Mirtazapine treatment after conditioning with methamphetamine alters subsequent expression of place preference. Drug Alcohol Depend. 2009 Jan 1;99(1-3):231-9.
13 Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91.
14 Activation of alpha1-adrenoceptors inhibits growth hormone secretion in humans. Exp Clin Endocrinol Diabetes. 2009 Oct;117(9):460-2.
15 Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
16 A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
17 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
18 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.
19 A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.
20 Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
21 Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716.
22 The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43.
23 Mechanisms of modafinil: A review of current research. Neuropsychiatr Dis Treat. 2007 June; 3(3): 349-364.
24 Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. Drugs. 2002;62(4):633-53.
25 Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses. Eur J Clin Pharmacol. 1996;49(5):411-5.
26 Induction of prostate apoptosis by alpha1-adrenoceptor antagonists: mechanistic significance of the quinazoline component. Prostate Cancer Prostatic Dis. 2002;5(2):88-95.
27 Bunazosin, a selective alpha1-adrenoceptor antagonist, as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage. Cardiovasc Drug Rev. 2005 Spring;23(1):43-56.
28 The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade. J Cardiovasc Pharmacol. 1984 Jan-Feb;6(1):142-50.
29 Antihypertensive action and blockade of alpha1-adrenoceptors by DL-017, a quinazoline derivative. J Cardiovasc Pharmacol. 2001 Dec;38(6):893-9.
30 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
31 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
32 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
33 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
34 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
35 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
36 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: 3639).
37 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
38 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
39 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
40 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
41 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
42 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
43 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
44 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
45 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
46 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
47 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
48 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
49 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.
50 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
51 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.
52 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.
53 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.
54 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.
55 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
56 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.
57 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.
58 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.
59 Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.
60 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
61 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
62 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
63 Alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog. J Pharmacol Exp Ther. 1997 Apr;281(1):337-46.
64 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.
65 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.
66 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.
67 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.
68 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.
69 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.
70 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.
71 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.