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
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]AF-DX 384
Ligand Kd (nM):
4.6
Ligand Concentration:
2 nM
Non Specific:
1 µM Atropine
Incubation:
60 min at RT
Control Inhibitor:
Methoctramine
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 final 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:
2
Turnaround Time
Standard:
10 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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