M3 Receptor Assay(s)

Background Information

Gi-coupled muscarinic receptor with presynaptic modulation of dopamine release in striatum. Relevant to schizophrenia (dopamine dysregulation), Parkinson"s psychosis, and cognitive disorders. Component of the xanomeline mechanism in KarXT. M4 positive allosteric modulators (PAMs) are an emerging antipsychotic strategy.

Family: GPCR
Protein Name: M3 Receptor
Gene Name: CHRM3

Organism: Human
Therapeutic Area: Metabolic, Respiratory

Assay Information

Validated Assay(s): Calcium Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: Panoptic
Plate Format: 384-well
Expression: Stable
Cell type: HEK293

Testing Information

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

Carbachol concentration-response curve for the human M3 muscarinic receptor using a fluorescence-based calcium assay in HEK293 cells.
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