M1 Receptor Assay(s)

Background Information

Gq-coupled muscarinic receptor driving the cognitive enhancement hypothesis in Alzheimer"s disease and a primary target in schizophrenia. M1/M4 dual agonism is the mechanism of xanomeline. KarXT (Cobenfy, xanomeline/trospium; AbbVie/Karuna) received FDA approval September 26, 2024 for schizophrenia — the first new antipsychotic mechanism in decades.

Family: GPCR
Protein Name: M1 Receptor
Gene Name: CHRM1

Organism: Human
Therapeutic Area: Neuropsychiatry, Neurodegeneration

Assay Information

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

Instrumentation: FLIPR
Plate Format: 384-well
Expression: Transient
Cell type: HEK293T

Testing Information

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

Carbachol concentration-response curve for the human M1 muscarinic receptor in a Brilliant Calcium fluorescence assay using HEK293T cells.
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