H3 Human Histamine GPCR Cell Based Antagonist Arrestin LeadHunter Assay - US

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.

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 β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Histamine

Class:

Class A

Coupling:

Gi/Go

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

Cell Type:

CHO-K1