Biological Information

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:

D3

Uniprot Number:

P35462

Gene Name:

DRD3

Gene ID:

1814

Accession Number:

NM_000796.3

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:

Dopamine

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:

Dopamine D3 receptor antagonism be useful in the treatment of psychosis, possibly without causing tardive dyskineasia, attention deficit disorder and hyperprolactineamia; receptor antagonism has also been reported to attenuate cocaine addiction.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA