kappa (KOP) Human Opioid GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Opiate receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Opiate receptors are found primarily, but not entirely, in the central nervous system. Opiate k receptor agonism may be analgesic, induce diuresis and reduce gastrointestinal transit.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
kappa (KOP) Human Opioid GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
333211-0
Protein
kappa (KOP)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
kappa (KOP) Human Opioid GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
333211-1
Protein
kappa (KOP)
Organism
Human
Assay Sub Type
Cell Based
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_000912.3
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant Opiate κ receptor expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1 x 10^5/ml) in modified HBSS pH 7.4 buffer at 37°C for 20 minutes. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥ 50%) relative to the 10 µM U69593 control response indicates possible opiate κ receptor agonist activity. Test compound-induced inhibition of the 5 nM U69593 induced cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
20 min at 37°C
Control Inhibitor:
nor-Binaltorphimine
Control Activator:
U-69593
Criteria For Significance:
≥ 50% decrease in cAMP relative to U-69593 response, ≥ 50% Inhibition of U-69593-induced cAMP decrease
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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