M2 Receptor Assay(s)

Background Information

Gi-coupled muscarinic receptor predominantly expressed in the sinoatrial and atrioventricular nodes of the myocardium, as well as presynaptic nerve terminals. Mediates parasympathetic (vagal) cardiac slowing via adenylyl cyclase inhibition and activation of inwardly rectifying GIRK (IKACh) potassium channels. In the CNS, functions as an inhibitory autoreceptor and heteroreceptor modulating neurotransmitter release.

Family: GPCR
Protein Name: M2 Receptor
Gene Name:CHRM2

Organism: Human
Therapeutic Area: Cardiovascular, Neuropsychiatry

Assay Information

Validated Assay(s): Gi/o GPCR-GIRK Thallium Flux Assay, APC
Assay type: Cell-based
Method: Fluorescence

Instrumentation: Flexstation
Plate Format: 96-well
Expression: Transient 
Cell type: HEK293

Testing Information

Functional Mode(s): Agonist
Reference compound(s): Carbachol

Acetylcholine concentration-response curve for the human M2 muscarinic receptor using a Gαi/o GPCR-GIRK thallium flux assay in HEK293 cells.
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