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.

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:

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

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