Biological Information
Background Information:
Muscarinic 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 widely distributed in the central and peripheral nervous system as well as various tissues.
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 β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.
Family:
GPCR
Sub Family:
Acetylcholine (Muscarinic)
Class:
Class A
Coupling:
Gi/Go
Protein Name:
M2
Uniprot Number:
P08172
Protein Aliases:
acetylcholine receptor, muscarinic 2
Gene Name:
CHRM2
Gene ID:
1129
Accession Number:
AF498916
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 Inhibitor:
Atropine
Control Activator:
Acetylcholine
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:
Muscarinic M2 subtype receptor agonism may cause bradycardia and hypotension. Receptor antagonism may cause airways hyper-reactivity and tachycardia.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA