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

General Information of Drug (ID: DM2QJKZ)

Drug Name

SB 258585 Drug Info

Synonyms

SB-258585; SB258585; SB-258,585; Tocris-1961; NCGC00025328-01; AC1MN2NM; SCHEMBL678180; CHEMBL60264; GTPL3232; CHEBI:93418; BDBM86428; ZINC3923836; NCGC00025328-02; BRD-K80639402-003-01-1; 4-iodo-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]benzenesulfonamide; 4-iodo-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]benzenesulfonamide; Benzenesulfonamide, 4-iodo-N-(4-methoxy-3-(4-methyl-1-piperazinyl)phenyl)-

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

PubChem CID: 3248571
ChEBI ID: CHEBI:93418
CAS Number: CAS 209480-63-7
TTD Drug ID: DM2QJKZ

Molecule-Related Drug Atlas

Molecule Type:

DTT

DOT

Drug Status:

Clinical Trial Drug(s)

Approved Drug(s)

Discontinued Drug(s)

Investigative Drug(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	[3]
SB-742457	DM6L4ZT	Alzheimer disease	8A20	Phase 3	[4]
AVN 211	DMVB4OS	Schizophrenia	6A20	Phase 2/3	[5]
SYN120	DMDF7XB	Parkinson disease	8A00.0	Phase 2	[6]
AVN 101	DMJFLBC	Alzheimer disease	8A20	Phase 2	[5]
SYN-120	DMPW0UL	Alzheimer disease	8A20	Phase 2	[7]
PF-05212377	DMPVQYR	Alzheimer disease	8A20	Phase 2	[8]
AVN 322	DMK2LGM	Cognitive impairment	6D71	Phase 2	[4]
SAM-531	DMHVJZ6	Alzheimer disease	8A20	Phase 2	[9]
SUVN-502	DMQD753	Alzheimer disease	8A20	Phase 2	[10]
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Drug(s) Affected By 5-hydroxytryptamine receptor 6 (HTR6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Clozapine	DMFC71L	Schizophrenia	6A20	Approved	[11]
Olanzapine	DMPFN6Y	Bipolar depression		Approved	[11]
Methamphetamine	DMPM4SK	Anxiety		Approved	[12]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[13]
LYSERGIC ACID DIETHYLAMIDE	DMACMLO	Addictive disorder	6C50-6C5Z	Withdrawn from market	[14]
Formaldehyde	DM7Q6M0	Discovery agent	N.A.	Investigative	[15]
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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 6 receptor (HTR6)	TTJS8PY	5HT6R_HUMAN	Antagonist	[2]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
5-hydroxytryptamine receptor 6 (HTR6)	OT8GTDDY	5HT6R_HUMAN	Protein Interaction/Cellular Processes	[2]

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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: 3232).
2	5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585. Synapse. 2002 Sep 1;45(3):191-9.
3	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.
4	5-HT6 receptors and Alzheimer's disease. Alzheimers Res Ther. 2013; 5(2): 15.
5	Latrepirdine, a potential novel treatment for Alzheimer's disease and Huntington's chorea. Curr Opin Investig Drugs. 2010 January; 11(1): 80-91.
6	Therapeutic strategies for Parkinson disease: beyond dopaminergic drugs. Nat Rev Drug Discov. 2018 Nov;17(11):804-822.
7	The Serotonin-6 Receptor as a Novel Therapeutic Target. Exp Neurobiol. 2011 December; 20(4): 159-168.
8	PF-05212377 Alzheimer's Disease (Phase 2). Pfizer.
9	Activation of 5-HT6 receptors modulates sleep-wake activity and hippocampal theta oscillation. ACS Chem Neurosci. 2013 Jan 16;4(1):191-9.
10	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.
11	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.
12	Serotonin 6 receptor gene is associated with methamphetamine-induced psychosis in a Japanese population. Drug Alcohol Depend. 2011 Jan 1;113(1):1-7. doi: 10.1016/j.drugalcdep.2010.06.021. Epub 2010 Aug 11.
13	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.
14	N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT?R) antagonists with unique structural features. J Med Chem. 2011 Oct 27;54(20):7030-54. doi: 10.1021/jm200466r. Epub 2011 Sep 26.
15	Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.