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

General Information of Drug (ID: DM8S593)

• Drug Name: Thioperamide Drug Info
• Synonyms: Thioperamide; 106243-16-7; Thioperamide maleate; MR 12842; UNII-II4319BWUI; 1-Piperidinecarbothioamide, N-cyclohexyl-4-(1H-imidazol-4-yl)-; II4319BWUI; N-Cyclohexy-4-(imidazol-4-yl)-1-piperidinecarbothioamide; CHEMBL260374; N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide; CHEBI:81391; N-Cyclohexyl-4-(1H-imidazol-5-yl)-1-piperidinecarbothioamide; Tocris-0644; Lopac-T-123; Lopac0_001214; SCHEMBL2235762; GTPL1267; AC1MI071; BDBM22914; DTXSID50147555; MolPort-023-275-907; MolPort-015-163-994

Indication

Disease Entry	ICD 11	Status	REF
Cognitive impairment	6D71	Terminated	[1]

• Cross-matching ID:
  PubChem CID: 3035905
  ChEBI ID: CHEBI:81391
  CAS Number: CAS 106243-16-7
  TTD Drug ID: DM8S593
  VARIDT Drug ID: DR00535

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine H4 receptor (H4R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-3893787	DMC2FAL	Atopic dermatitis	EA80	Phase 2	[4]
JNJ-38518168	DM9UMIO	Plaque psoriasis	EA90.0	Phase 2	[5]
UR-63325	DME6X27	Allergic rhinitis	CA08.0	Phase 2	[6]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole	DMZVBPG	Discovery agent	N.A.	Investigative	[7]
impromidine	DMTDRPM	Discovery agent	N.A.	Investigative	[8]
burimamide	DMZ2VYG	Discovery agent	N.A.	Investigative	[9]
Imetit	DMMJ6NS	Discovery agent	N.A.	Investigative	[10]
[125I]iodophenpropit	DMN4ABU	Discovery agent	N.A.	Investigative	[11]
(R)-alpha-methylhistamine	DMKAW4P	Discovery agent	N.A.	Investigative	[12]
N-[3H]alpha-methylhistamine	DMWDCV1	Discovery agent	N.A.	Investigative	[13]

Drug(s) Targeting Histamine H3 receptor (H3R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pitolisant	DM8RFNJ	Excessive daytime sleepiness	MG42	Approved	[14]
SUVN-G3031	DM3BO8G	Cognitive impairment	6D71	Phase 3	[15]
JNJ-17216498	DM1GRCU	Narcolepsy	7A20	Phase 2	[16]
GSK239512	DMBJMZC	Alzheimer disease	8A20	Phase 2	[17]
JNJ-39220675	DM0WY3H	Alcohol dependence	6C40.2	Phase 2	[18]
AZD-5213	DMOZ04X	Alzheimer disease	8A20	Phase 2	[19]
Bavisant	DM6CVZ5	Attention deficit hyperactivity disorder	6A05.Z	Phase 2	[20]
ABT-288	DM7X54F	Alzheimer disease	8A20	Phase 2	[21]
SAR-110894	DMCLEXM	Alzheimer disease	8A20	Phase 2	[19]
ABT-652	DMLEO2Z	Diabetic neuropathy	8C0Z	Phase 2	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H3 receptor (H3R)	TT9JNIC	HRH3_HUMAN	Antagonist	[2]
Histamine H4 receptor (H4R)	TTXJ178	HRH4_HUMAN	Antagonist	[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: 1267).
• [2] The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
• [3] Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86.
• [4] Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6596-602.
• [5] The histamine H4 receptor: from orphan to the clinic. Front Pharmacol. 2015; 6: 65.
• [6] Azines as histamine H4 receptor antagonists. Front Biosci (Schol Ed). 2012 Jan 1;4:967-87.
• [7] Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. Bioorg Med Chem. 2010 Jul 15;18(14):5441-8.
• [8] Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first pote... J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21.
• [9] Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. J Pharmacol Exp Ther. 2001 Oct;299(1):121-30.
• [10] Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. J Neurophysiol. 2006 Apr;95(4):2492-500.
• [11] Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. J Med Chem. 2008 Jun 12;51(11):3145-53.
• [12] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [13] Histamine induces cytoskeletal changes in human eosinophils via the H(4) receptor. Br J Pharmacol. 2003 Nov;140(6):1117-27.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [16] Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
• [17] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [18] JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41.
• [19] SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
• [20] Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
• [21] A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
• [22] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)