H4 Human Histamine GPCR GTPgammaS Agonist LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
All histamine receptor subtypes are members of the superfamily of G protein-coupled receptors. Generally, histamine modulates inflammatory and allergic responses via H1 receptors, gastric acid secretion through H2 receptors, and neurotransmitter release in the central nervous system via H3 receptors. The H4 receptor mRNA is expressed in a variety of cell types, including peripheral blood mononuclear cells, neutrophils, eosinophils, mast cells, and resting CD4+ 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
Gene Name:
HRH4
Gene ID:
59340
Gene Aliases:
H4R|HH4R|AXOR35|GPCR105|GPRv53
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
HEK293
Assay Information
Assay Type:
Functional
Assay Sub Type:
GTPgammaS
Functional Mode:
Agonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant histamine H4 receptor expressed in HEK-293 cells are used. Test compound and/or vehicle is preincubated with the membranes (0.3 mg/ml) and 10 μM GDP in modified HEPES pH 7.4 buffer for 20 minutes and SPA beads are then added for another 60 minutes at 30°C. The reaction is initiated by 0.3 nM [35S]GTPγS for an additional 30 minutes incubation period. Test compound-induced increase of [35S]GTPγS binding by 50 percent or more (≥50%) relative to the 10 μM 4-Methylhistamine response indicates possible histamine H4 receptor agonist activity. Test compound-induced inhibition of 0.2 μM 4-Methylhistamine-induced increase of [35S]GTPγS binding response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 30°C
Control Activator:
4-Methylhistamine
Criteria For Significance:
≥ 50% Increase in bound [35γS]GTPgammaS relative to 4-Methylhistamine response, ≥ 50% Inhibition of 4-Methylhistamine-induced bound [35S]GTPgammaS
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 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:
Taiwan - Taipei
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