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Cholinergic receptor, muscarinic 1 (M1) - CHRM1

Target Class GPCR FamilyAcetylcholine
SpeciesHuman   
Background
The muscarinic cholinergic receptors belong to a larger family of G protein-coupled receptors. The functional diversity of these receptors is defined by the binding of acetylcholine and includes cellular responses such as adenylate cyclase inhibition, phosphoinositide degeneration, and potassium channel mediation. Muscarinic receptors influence many effects of acetylcholine in the central and peripheral nervous system. The muscarinic cholinergic receptor 1 is involved in mediation of vagally-induced bronchoconstriction and in the acid secretion of the gastrointestinal tract. The gene encoding this receptor is localized to 11q13. [provided by RefSeq, Jul 2008]

Cell Background
U2OS
Readout
Calcium
Method
Detect calcium mobilization using DiscoverX Calcium No WashPLUS
Agonist/Ligand
Acetylcholine
Agonist/Ligand EC50
12
Agonist Effect (Activation)
proconvulsant; increase gastric acid secretion; hypertension; tachycardia; hyperthermia
Antagonist Effect (Inhibition)
decrease cognitive function; decrease gastric acid secretion; blurred vision
Ref.
Bowes et. al. 2012
AgonistEC50(nM)
Acetylcholine12
Oxotremorine10
Xanomeline 10
Cells are plated in a 384-well plate and incubated overnight at 37°C/5% CO2 to allow the cells to attach and grow. Cells are then stimulated with a control agonist. Following stimulation, calcium mobilization is detected using the Calcium No WashPLUS detection kit.
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