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Application: Screen for activators or inhibitors for M3 receptor-related research and drug discovery.Counter-screen functionally selective agonists or biased agonists for M1 and M5 receptors.Characterize mAChR M3 antibodies/antagonists and agonists of binding assay.
Background: Muscarinic acetylcholine receptors (mAChRs) are relatively abundant and mediate many of the diverse actions of acetylcholine in the CNS (central nervous system), as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. They are involved in regulating a large number of cognitive, behavioral, motor, and autonomic functions. There are five muscarinic receptor subtypes referred to as M1, M2, M3, M4 and M5 which belong to the GPCR (G-protein-coupled receptor) superfamily. M1, M3 and M5 receptor subtypes couple efficiently through Gq/11, to activate phospholipase C (PLC), which initiates the phosphatidylinositol (IP3) turnover response and leads to the release of intracellular calcium ions (Ca2+). The M2 and M4 receptor subtypes preferentially couple to Gi/o G-proteins and inhibit adenylyl cyclase (AC) activity, which leads to a decrease in the level of cAMP. M2 and M4 receptors also activate G protein-coupled potassium channel by βγ-dimer dissociated from the active Gi/o G-protein, which leads to hyperpolarization of the plasma membrane of excitable cells. The disruption of muscarinic signaling frequently contributes to several pathophysiological conditions in the CNS and in the periphery. Thus, muscarinic agonists have a wide therapeutic potential in the treatment of neurodegenerative and neuropsychiatric disorders and conditions, e.g. Alzheimer's disease, schizophrenia, pain, and ischemia or heart failure. To target these diseases, selective modulation of individual muscarinic receptor subtypes is necessary to avoid undesired side effects. The orthosteric binding site of all subtypes of muscarinic receptors is virtually the same and no affinity-based selective agonists of muscarinic receptors have been discovered so far. The development of biased agonists can be the right approach to achieve selective modulation of individual subtypes of muscarinic receptors.
Description: The Muscarinic Acetylcholine Receptor (mAChR) M3/NFAT Luciferase Reporter HEK293 Cell Line is a HEK293 cell line expressing the full-length human muscarinic acetylcholine receptor M3 (CHRM3/M3R/M3; accession number: NM_000740.3) and a firefly luciferase reporter under the control of the NFAT (nuclear factor of activated T cells) response element.This cell line has been validated by flow cytometry and for its responses to the muscarinic acetylcholine receptor agonists Oxotremorine M and Carbamoylcholine chloride (carbachol). Luciferase activity increases in proportion to mAChR activation.
Genbank: NM_000740.3
Host Cell Line: HEK293, epithelial-like cells, adherent
Mycoplasma Testing: The cell line has been screened to confirm the absence of Mycoplasma species.
Storage Stability: Cells are shipped in dry ice and should immediately be thawed or stored in liquid nitrogen upon receipt. Do not use a -80°C freezer for long term storage.
Uniprot: P20309
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: BSL-2
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