Biological Information

Background Information:

Orphanin (N/OFG, NOP) 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. The neuropeptide nociceptin/Orphanin FQ (N/OFQ) was recently identified as the endogenous ligand for the opioid receptor-like (ORL1) receptor. Orphanin ORL1 receptors are found primarily, but not entirely, in the central nervous system.

Family:

GPCR

Sub Family:

Opioid

Class:

Class A

Protein Name:

NOP (ORL1)

Uniprot Number:

P41146

Protein Aliases:

LC132 receptor-like|orphanin FQ receptor|kappa3-related opioid receptor|nociceptin/orphanin FQ receptor

Gene Name:

OPRL1

Gene ID:

4987

Gene Aliases:

NOCIR|ORL1|OOR|KOR-3|NOPr

Accession Number:

NM_182647

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

20 min at 37°C

Control Inhibitor:

UFP-101

Control Activator:

nociceptin (0.3 nM)

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 finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5284596

Name

Naloxone

Measurement

- IC50

PubChem ID

5311339

Name

JTC-801

Measurement

2500nM - IC50

PubChem ID

5497186

Name

Naltrindole

Measurement

8900nM - IC50

PubChem ID

25081457

Name

UFP-101

Measurement

44nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Orphanin ORL1 receptor agonism may cause nociception or analgesia, be anxiolytic, impair memory and learning, inhibit neurogenic urinary incontinence, increase food intake and reduce gastrointestinal transit.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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