M5 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. A muscarinic M5 subtype antagonist may reduce dopamine D1 central nervous stimulation and inhibit salivary secretion.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
M5 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
332150-0
Protein
M5
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
M5 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
332150-1
Protein
M5
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Acetylcholine (Muscarinic)
Class:
Class A
Protein Name:
M5
Uniprot Number:
P08912
Protein Aliases:
acetylcholine receptor, muscarinic 5
Gene Name:
CHRM5
Gene ID:
1133
Accession Number:
NM_001320917
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 M5 receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1.5 x 10^6 /ml) in stimulation buffer of IP1 Tb kit for 30 minutes at 37°C. Test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 100 μM acetylcholine chloride response indicates possible M5 receptor agonist activity. Test compound-induced inhibition of 10 μM acetylcholine chloride-induced increase of fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 37°C
Control Inhibitor:
Atropine
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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
M5 Human Acetylcholine (Muscarinic) GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
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M5 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
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