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.
cAMP Hunter cell lines overexpress naturally coupled, wild type GPCRs and are designed to detect increases in intracellular cAMP levels (Gs-coupled receptors) or inhibition of intracellular cAMP production (Gi-coupled receptors) in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit. cAMP Hunter cell lines expressing receptors that will couple to Gq proteins can also be used to detect induction of calcium mobilization.
Family:
GPCR
Sub Family:
Histamine
Class:
Class A
Coupling:
Gq & Gs
Protein Name:
H2
Uniprot Number:
P25021
Protein Aliases:
HH2R|Gastric receptor I
Gene Name:
HRH2
Gene ID:
3274
Accession Number:
AY136744
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Testing Information
Control Inhibitor:
Tiotidine
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 H2 receptor antagonism is used primarily in the treatment of peptic ulcers and gastroeosophageal reflux disease (GERD); reduction of gastric acid secretion may alter bioavailability and rate of absorption of some therapeutic agents.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA