mu (MOP) Human Opioid GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW

Item: 333310-1

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OVERVIEW

DOCUMENTS/REFERENCES

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:

mu (MOP)

Uniprot Number:

P35372

Protein Aliases:

MOR-1|Mu opiate receptor|Mu opioid receptor|MOP|hMOP

Gene Name:

OPRM1

Gene ID:

4988

Gene Aliases:

MOR1

Accession Number:

NM_000914

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

Naltrexone

Criteria For Significance:

≥ 50% decrease in cAMP relative to DAMGO response, ≥ 50% Inhibition of DAMGO-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:

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

5284596

Name

Naloxone

Measurement

0.018μM - IC50

PubChem ID

5360515

Name

Naltrexone

Measurement

0.0031μM - IC50

PubChem ID

5497186

Name

Naltrindole

Measurement

0.086μM - IC50

PubChem ID

101834975

Name

CTOP

Measurement

1μM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Opioid receptor agonists may be analgesic, reduce gastrointestinal transit, adversely affect respiration and become addictive.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei