D2S Human Dopamine GPCR Cell Based Agonist Arrestin LeadHunter Assay - US

Background Information:

Five subtypes of dopamine receptors, D1, D2, D3, D4 and D5, were identified on the basis of pharmacological or biochemical criteria. The D2-like receptors include the two isoforms of the D2 receptor, differing in the length of their predicted third cytoplasmic loop, dubbed D2 short (D2S) and D2 long (D2L). The dopamine D2S receptor couples to PTX-sensitive G proteins (Gi/o) to initiate multiple signaling pathways. In cells of neuroendocrine origin, the D2S couples to "inhibitory" pathways, including inhibition of adenylyl cyclase, activation of potassium channels to hyperpolarize the cell membrane, and inhibition of L-type calcium channels, which in concert mediate inhibition of hormone secretion and gene transcription, and inhibition of cell proliferation. D2 dopamine receptors have been implicated in the pathophysiology of schizophrenia and Parkinson’s disease.

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:

D2

Uniprot Number:

P14416

Gene Name:

DRD2

Gene ID:

1813

Accession Number:

NM_016574.3

Organism:

Human

Cell Type:

CHO-K1