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