Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01193

Target Information
NameHistamine H4 receptor    
Type of targetResearch target    
SynonymsAXOR35    
G protein-coupled receptor 105    
GPCR105    
GPRv53    
H4 receptor    
HH4R    
SP9144    
DiseaseAllergic diseases
[ICD9: 995.3   ICD10: T78.4]
[1]
Allergy, unspecified
[ICD9: 995.3   ICD10: T78.4]
[2]
Asthma
[ICD9: 493   ICD10: J45]
[2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDQ9H3N8
FunctionThe H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues and display a significant level of constitutive activity (spontaneous activity in the absence of agonist).    
SequenceMPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAIS DFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAV SYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSF LEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSA STEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARR LAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPL CHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (1H-indol-2-yl)[3]
(R)-[4]
(R)-3-[5]
4- (2-[6]
6- (4-Methylpiperazin-1-yl)-9H-purin-2-amine[7]
6- (4-Methylpiperazin-1-yl)pyrimidine-2,4-diamine[7]
6- (4-methylpiperazin-1-yl)-9Hpurine[7]
9-benzyl-6- (4-methylpiperazin-1-yl)-9H-purine[7]
A-846714[8]
A-943931[8]
IODOPHENPROPIT[4]
JNJ-7777120[9]
JNJ-7777120[7]
AgonistClobenpropit[10][11]
Imetit[12][13]
N-alpha-methyl histamine[1]
R-alpha-methyl histamine[1]
AntagonistThioperamide[14][15][16]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Histamine induces cytoskeletal changes in human eosinophils via the H(4) receptor. Br J Pharmacol. 2003 Nov;140(6):1117-27. Epub 2003 Oct 6. To Reference
Ref 2Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6. To Reference
Ref 3J Med Chem. 2005 Dec 29;48(26):8289-98.Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. To Reference
Ref 4J Med Chem. 2008 Jun 12;51(11):3145-53. Epub 2008 May 7.Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. To Reference
Ref 5Bioorg Med Chem Lett. 2009 Dec 1;19(23):6682-5. Epub 2009 Oct 6.Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. To Reference
Ref 6Bioorg. Med. Chem. 18(14):5441-5448 (2010) To Reference
Ref 7Bioorg Med Chem. 2009 Oct 15;17(20):7186-96. Epub 2009 Sep 2.2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. To Reference
Ref 8J Med Chem. 2008 Oct 23;51(20):6547-57. Epub 2008 Sep 26.Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. To Reference
Ref 9Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9. Epub 2010 Mar 3.Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. To Reference
Ref 10Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. Bioorg Med Chem. 2009 Jun 1;17(11):3987-94. Epub 2009 Apr 11. To Reference
Ref 11The histamine H4 receptor is functionally expressed on T(H)2 cells. J Allergy Clin Immunol. 2009 Mar;123(3):619-25. To Reference
Ref 12Histamine excites neonatal rat sympathetic preganglionic neurons in vitro via activation of H1 receptors. J Neurophysiol. 2006 Apr;95(4):2492-500. Epub 2005 Dec 14. To Reference
Ref 13Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol. 2004 May;142(1):161-71. To Reference
Ref 14Role of histamine in short- and long-term effects of methamphetamine on the developing mouse brain. J Neurochem. 2008 Nov;107(4):976-86. Epub 2008 Sep 11. To Reference
Ref 15Role of histamine H3 and H4 receptors in mechanical hyperalgesia following peripheral nerve injury. Neuroimmunomodulation. 2007;14(6):317-25. Epub 2008 Apr 10. To Reference
Ref 16The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20. To Reference



 

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