Biological Information

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.

cAMP Hunter™ Gi cell lines overexpress naturally Gi coupled, wildtype GPCRs and are designed to detect inhibition of intracellular cAMP production 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.

Family:

GPCR

Sub Family:

Dopamine

Class:

Class A

Coupling:

Gi/Go

Protein Name:

D2

Uniprot Number:

P61169

Gene Name:

DRD2

Gene ID:

24318

Accession Number:

NM_012547.1

Organism:

Rat

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

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 D2 receptor antagonist may be used in the treatment of psychosis; may also result in tardive dyskinesia and increase pituitary hormone secretion.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA