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:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
Chem-1
Assay Information
Assay Type:
Functional
Assay Sub Type:
GTPgammaS
Functional Mode:
Agonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Incubation:
30 min at 30°C
Control Activator:
U-69593
Criteria For Significance:
≥ 50% Increase in bound [35S]GTPgammaS relative to U-69593 response, ≥ 50% Inhibition of U-69593-induced bound [35S]GTPgammaS
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
Adverse / Beneficial Action:
Opioid receptor agonist may be analgesic, induce diuresis, reduce gastrointestinal transit.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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