Biological Information

Background Information:

Motilin 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. Muscarinic receptors are primarily distributed in the gastrointestinal tract and may also be present in the central nervous system.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Motilin

Class:

Class A

Coupling:

Gq

Protein Name:

Motilin

Uniprot Number:

O43193

Gene Name:

MLNR

Gene ID:

2862

Gene Aliases:

GPR38|MTLR|MTLR1

Accession Number:

AY603964

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

β-Arrestin Isoform:

β-Arrestin-2

Testing Information

Control Activator:

motilin

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:

Motilin receptor agonism may accelerate gastric emptying and intestinal motility, which may be associated with nausea.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA