M3 Human Acetylcholine (Muscarinic) GPCR Binding Antagonist Radioligand LeadHunter Assay - FR

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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:

Uniprot Number:

P20309

Protein Aliases:

acetylcholine receptor, muscarinic 3

Gene Name:

CHRM3

Gene ID:

1131

Accession Number:

NM_000740

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]4-DAMP

Ligand Kd (nM):

0.5

Ligand Concentration:

0.2 nM

Non Specific:

1 µM Atropine

Incubation:

60 min at RT

Control Inhibitor:

4-Damp methiodide

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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

4848

Name

Pirenzepine

Measurement

75nM - IC50

PubChem ID

174174

Name

Atropine

Measurement

0.4nM - IC50

PubChem ID

3014059

Name

4-Damp methiodide

Measurement

1.19nM - IC50

PubChem ID

44134815

Name

Methoctramine

Measurement

170nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

A muscarinic M3 subtype receptor antgonist may reduce bronchial tone in chronic obstructive pulmonary disease (COPD) and asthma, gastrointestinal motility as well as interfere with ocular accommodation and outflow facility.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault