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 central nervous system, is released following a circadian rhythm with high levels at night.. It is also a highly potent antioxidative substance, reducing the damage caused by free radicals generated by light and beta-amyloid peptide.

cAMP Hunter™ Gi cell lines overexpress naturally Gi coupled, wild type GPCRs and are designed to detect inhibition of intracellular cAMP production in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.

Family:

GPCR

Sub Family:

Melatonin

Class:

Class A

Coupling:

Gi/Go

Protein Name:

MT1

Uniprot Number:

P48039

Protein Aliases:

Mel1a receptor

Gene Name:

MTNR1A

Gene ID:

4543

Gene Aliases:

MEL-1A-R

Accession Number:

NM_005958

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Testing Information

Control Activator:

2-iodomelatonin

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

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:

USA - Fremont, CA