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

PubChem ID

105104

Name

U-69593

Measurement

5.3nM - EC50

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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