Biological Information

Background Information:

Opiates exert their effects in the central and peripheral nervous systems through interaction with m, k and d, three major types of opioid receptors, which are structural homologues and belong to the G protein-coupled receptor (GPCR) family. G-protein cascades activated by these three receptors can reduce adenylyl cyclase activity, alter inositol trisphosphate turnover, activate G-protein-linked, inward potassium channels, and close calcium channels. These receptors mediate the actions of opiate drugs and endogenous opioid neuropeptides in producing euphoria, modulating pain perception, and altering other important functions in the central and peripheral nervous systems. Opioid analgesics provide symptomatic relief of pain, cough and diarrhea.

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:

Opioid

Class:

Class A

Coupling:

Gi/Go

Protein Name:

delta (DOP)

Uniprot Number:

P41143

Protein Aliases:

DOR-1

Gene Name:

OPRD1

Gene ID:

4985

Gene Aliases:

OPRD

Accession Number:

NM_000911

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

β-Arrestin Isoform:

β-Arrestin-2

Testing Information

Control Inhibitor:

Naltriben mesylate

Control Activator:

DADLE

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:

Opiate d receptor agonism may be analgesic and reduce gastrointestinal transit

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA