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
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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