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

General Information of Drug (ID: DMD8CQS)

Drug Name

2-methylhistamine Drug Info

Synonyms

56975-07-6; Tetrahydro-5-(2-hydroxyethyl)-1,3-bis(hydroxymethyl)-1,3,5-triazine-2(1H)-thione; 5-(2-hydroxyethyl)-1,3-bis(hydroxymethyl)-1,3,5-triazinane-2-thione; EINECS 260-494-0; AC1L3OH4; GTPL1268; AC1Q7F21; CTK5A6094; DTXSID70205580; 1,3,5-Triazine-2(1H)-thione,tetrahydro-5-(2-hydroxyethyl)-1,3-bis(hydroxymethyl)-

Indication

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

Cross-matching ID

PubChem CID: 91613
ChEBI ID: CHEBI:74761
CAS Number: CAS 34392-54-6
TTD Drug ID: DMD8CQS

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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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	[3]
JNJ-38518168	DM9UMIO	Plaque psoriasis	EA90.0	Phase 2	[4]
UR-63325	DME6X27	Allergic rhinitis	CA08.0	Phase 2	[5]
Thioperamide	DM8S593	Cognitive impairment	6D71	Terminated	[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]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H4 receptor (H4R)	TTXJ178	HRH4_HUMAN	Agonist	[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: 1268).
2	Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br J Pharmacol. 2006 Apr;147(7):744-54.
3	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.
4	The histamine H4 receptor: from orphan to the clinic. Front Pharmacol. 2015; 6: 65.
5	Azines as histamine H4 receptor antagonists. Front Biosci (Schol Ed). 2012 Jan 1;4:967-87.
6	Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86.
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.