D4 Human Dopamine GPCR Cell Based Agonist Arrestin LeadHunter Assay - US

Background Information:

Dopamine 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. Various members of the dopamine receptor family are generally classified as either ‘D1-like’ or ‘D2-like’. D2-like receptors comprise the D2, D3 and D4 receptors, which inhibit activation of adenylate cyclases via coupling to G1/G0 protein.

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:

Dopamine

Class:

Class A

Coupling:

Gi/Go

Protein Name:

D4

Uniprot Number:

P21917

Gene Name:

DRD4

Gene ID:

1815

Gene Aliases:

DRD1B

Accession Number:

NM_000797.2

Organism:

Human

Cell Type:

CHO-K1