H3 Human Histamine GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
OVERVIEW
DOCUMENTS/REFERENCES
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 H3 receptors on nerve terminals function as feedback inhibitors in a wide variety of organ systems.
Family:
GPCR
Sub Family:
Histamine
Class:
Class A
Protein Name:
H3
Uniprot Number:
Q9Y5N1
Protein Aliases:
HH3R|G-protein coupled receptor 97
Gene Name:
HRH3
Gene ID:
11255
Gene Aliases:
GPCR97
Accession Number:
NM_007232
Organism:
Human
Construct Details:
Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
HTRF
Testing Information
Incubation:
10 min at 37°C
Control Inhibitor:
thioperamide
Control Activator:
histamine (1000 nM)
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 finµL 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:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Adverse / Beneficial Action:
Histamine H3 receptors are presynaptic receptors present on histaminergic nerve terminals in the CNS that exert feedback regulation of histamine synthesis and release.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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