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

PubChem ID

774

Name

Histamine

Measurement

22nM - IC50

PubChem ID

2756

Name

Cimetidine

Measurement

51000nM - IC50

PubChem ID

3692

Name

Imetit

Measurement

4.28nM - IC50

PubChem ID

156615

Name

(R)-alpha-Methylhistamine

Measurement

520nM - IC50

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

RELATED SOLUTIONS

Item: P22-p