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:
M4
Uniprot Number:
P08173
Protein Aliases:
acetylcholine receptor, muscarinic 4
Gene Name:
CHRM4
Gene ID:
1132
Accession Number:
NM_000741
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
GTPgammaS
Functional Mode:
Agonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Incubation:
15 min at 30°C
Control Activator:
McN-A-343
Criteria For Significance:
≥ 50% Increase in bound [35S]GTPgammaS relative to McN-A-343 response, ≥ 50% Inhibition of McN-A-343-induced bound [35S]GTPgammaS
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
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