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.
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.
Family:
GPCR
Sub Family:
Histamine
Class:
Class A
Coupling:
Gq
Protein Name:
H1
Uniprot Number:
P35367
Protein Aliases:
HH1R
Gene Name:
HRH1
Gene ID:
3269
Accession Number:
AY136743
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
β-Arrestin Isoform:
β-Arrestin-2
Testing Information
Control Activator:
Histamine
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 10 concentrations are selected
Test Sample Requirements:
40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)
Minimum Order Quantity:
20
Turnaround Time
Standard:
15 Business Days
Clinical Relevance
Adverse / Beneficial Action:
Histamine H1 receptor antagonism is used in the treatment of various immediate hypersensitivity reactions; action upon the central nervous system may cause sedation while high doses may result in convulsions, especially in infants.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA