M2 Human Acetylcholine (Muscarinic) GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
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.
Family:
GPCR
Sub Family:
Acetylcholine (Muscarinic)
Class:
Class A
Protein Name:
M2
Uniprot Number:
P08172
Protein Aliases:
acetylcholine receptor, muscarinic 2
Gene Name:
CHRM2
Gene ID:
1129
Accession Number:
XM_011515769
Organism:
Human
Construct Details:
Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
HTRF
Testing Information
Incubation:
10 min at 37°C
Control Inhibitor:
Methoctramine
Control Activator:
acetylcholine (300 nM)
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Adverse / Beneficial Action:
Muscarinic M2 subtype receptor agonism may cause bradycardia and hypotension. Receptor antagonism may cause airways hyper-reactivity and tachycardia.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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