Biological Information

Background Information:

Melatonin 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. Melatonin, present primarily in the central nervous system, is released following a circadian rhythm with high levels at night.

Family:

GPCR

Sub Family:

Melatonin

Class:

Class A

Protein Name:

MT1

Uniprot Number:

P48039

Protein Aliases:

Mel1a receptor

Gene Name:

MTNR1A

Gene ID:

4543

Gene Aliases:

MEL-1A-R

Accession Number:

XM_011532002

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]2-iodomelatonin

Ligand Kd (nM):

0.04

Ligand Concentration:

0.01 nM

Non Specific:

1 µM Melatonin

Incubation:

240 min at RT

Control Inhibitor:

melatonin

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:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

905

Name

Melatonin

Measurement

0.15nM - IC50

PubChem ID

1858

Name

6-chloromelatonin

Measurement

0.56nM - IC50

PubChem ID

115348

Name

2-iodomelatonin

Measurement

0.095nM - IC50

PubChem ID

122162

Name

Luzindole

Measurement

87nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Melatonin MT1 receptor agonist is of potential therapeutic interest for the treatment of insomnia and circadian rhythm disruption and may be of benefit for the treatment on Alzheimers disease.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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