M3 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Muscarinic receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Muscarinic receptors are widely distributed in the central and peripheral nervous system as well as various tissues.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
M3 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
331950-0
Protein
M3
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
M3 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
331950-1
Protein
M3
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Acetylcholine (Muscarinic)
Class:
Class A
Protein Name:
M3
Uniprot Number:
P20309
Protein Aliases:
acetylcholine receptor, muscarinic 3
Gene Name:
CHRM3
Gene ID:
1131
Accession Number:
NM_000740
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant muscarinic M3 receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1 x 10^6/ml) in stimulation buffer of IP1 Tb kit for 45 minutes at 37°C. Test compound-induced increase of IP1 by 50 percent or more (≥50%) relative to the 100 μM Acetylcholine response indicates possible M3 receptor agonist activity. Test compound-induced inhibition of 30 μM Acetylcholine-induced increase of IP1 response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
45 min at 37°C
Control Inhibitor:
J 104129
Control Activator:
Acetylcholine
Criteria For Significance:
≥ 50% increase in IP-one relative to Acetylcholine response, ≥ 50% inhibition of Acetylcholine-induced response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
A muscarinic M3 subtype antgonist may reduce bronchocontriction and gastrointestinal motility as well as interfere with ocular accommodation and outflow facility.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
M3 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item: 331950-0
M3 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
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