NT1 Human Neurotensin GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Neurotensin (NT) receptors belong to the superfamily of G protein-coupled receptors. Neurotensin NT1 an NT2 receptors have seven transmembrane domains, whereas NT3 has a single transmembrane domain. 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. Neurotensin NT receptors are widely distributed in the central nervous system and gastrointestinal tract.

Family:

GPCR

Sub Family:

Neurotensin

Class:

Class A

Protein Name:

NT1

Uniprot Number:

P30989

Protein Aliases:

NTR1|High-affinity levocabastine-insensitive neurotensin receptor|NTRH

Gene Name:

NTSR1

Gene ID:

4923

Gene Aliases:

NTR|NTRR

Accession Number:

XM_011528827

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]Tyr3-neurotensin

Ligand Kd (nM):

0.22

Ligand Concentration:

0.05 nM

Non Specific:

1 µM Neurotensin

Incubation:

60 min at 4°C

Control Inhibitor:

neurotensin

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 final 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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

54385

Name

levocabastine

Measurement

- IC50

PubChem ID

5311451

Name

SR142948A

Measurement

1.8nM - IC50

PubChem ID

9940301

Name

Neuromedin N

Measurement

4.4nM - IC50

PubChem ID

90488724

Name

Neurotensin

Measurement

0.3nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Neurotensin NT1 receptor agonism may be useful in the treatment of schizophrenia, may increase gastric emptying and colonic propulsion as well as cardiac stimulation, cell proliferation and mast cell secretion.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault