Biological Information
Background Information:
Histamine receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Histamine receptors are found in most peripheral tissue and within the central nervous system. Histamine H4 receptors are present in a variety of cell types, including peripheral blood mononuclear cells, neutrophils, eosinophils and mast cells. These findings are highly suggestive of a role for the H4 receptor in immune and/or inflammatory modulation.
Family:
GPCR
Sub Family:
Histamine
Class:
Class A
Protein Name:
H4
Uniprot Number:
Q9H3N8
Protein Aliases:
HH4R|AXOR35|G-protein coupled receptor 105|GPRv53|Pfi-013|SP9144
Gene Name:
HRH4
Gene ID:
59340
Gene Aliases:
H4R|HH4R|AXOR35|GPCR105|GPRv53
Accession Number:
NM_021624
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]histamine
Ligand Kd (nM):
7.6
Ligand Concentration:
10 nM
Non Specific:
1 µM Imetit
Incubation:
60 min at RT
Control Inhibitor:
imetit
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Adverse / Beneficial Action:
Histamine H4 receptor antagonist may be useful in the treatment of allergy, asthma and inflammation.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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