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.

Family:

GPCR

Sub Family:

Opioid

Class:

Class A

Protein Name:

kappa (KOP)

Uniprot Number:

P41145

Protein Aliases:

KOR-1

Gene Name:

OPRK1

Gene ID:

4986

Gene Aliases:

KOR|OPRK

Accession Number:

NM_001282904

Organism:

Rat

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]U 69593

Ligand Kd (nM):

2

Ligand Concentration:

1 nM

Non Specific:

10 µM Naloxone

Incubation:

60 min at RT

Control Inhibitor:

U 50488 hydrochloride

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

2000nM - IC50

PubChem ID

3036289

Name

U-50488

Measurement

0.84nM - IC50

PubChem ID

5284596

Name

Naloxone

Measurement

5nM - IC50

PubChem ID

5462471

Name

DAMGO

Measurement

64nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Opioid receptor agonist may be analgesic, induce diuresis, reduce gastrointestinal transit.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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