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

General Information of Drug (ID: DM260RG)

• Drug Name: 2-(3-bromophenyl)histamine Drug Info
• Synonyms: 2-(3-Bromophenyl)histamine; CHEMBL26116; GTPL1194; SCHEMBL15974857; BDBM22863; PDSP2_001292; PDSP1_001308; AKOS022562838; AKOS023977997; 2-(3-Bromophenyl)-1H-imidazole-4-(ethanamine); 2-[2-(3-bromophenyl)-3H-imidazol-4-yl]ethanamine

Indication

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

• Cross-matching ID:
  PubChem CID: 23786499
  TTD Drug ID: DM260RG

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]
Thioperamide	DM8S593	Cognitive impairment	6D71	Terminated	[7]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole	DMZVBPG	Discovery agent	N.A.	Investigative	[8]
impromidine	DMTDRPM	Discovery agent	N.A.	Investigative	[3]
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]

Drug(s) Targeting Histamine H1 receptor (H1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[12]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[13]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[14]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[15]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[16]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[14]
Doxepin	DMPI98T	Anxiety		Approved	[17]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[14]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[18]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Agonist	[2]
Histamine H4 receptor (H4R)	TTXJ178	HRH4_HUMAN	Agonist	[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: 1194).
• [2] Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. J Pharmacol Exp Ther. 2003 Jun;305(3):1104-15.
• [3] 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.
• [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] Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86.
• [8] 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.
• [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] 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.
• [14] 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.
• [15] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [16] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [17] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [18] 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.
• [19] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.