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.

Family:

GPCR

Sub Family:

Opioid

Class:

Class A

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

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]DADLE

Ligand Kd (nM):

0.6

Ligand Concentration:

0.5 nM

Non Specific:

10 µM Naltrexone

Incubation:

60 min at RT

Control Inhibitor:

DPDPE

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

104787

Name

DPDPE

Measurement

3.3nM - IC50

PubChem ID

5284596

Name

Naloxone

Measurement

99nM - IC50

PubChem ID

5462471

Name

DAMGO

Measurement

1500nM - IC50

PubChem ID

91826457

Name

U 50488 hydrochloride

Measurement

43500nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Opiate d receptor agonism may be analgesic and reduce gastrointestinal transit

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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