M5 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. A muscarinic M5 subtype antagonist may reduce dopamine D1 central nervous stimulation and inhibit salivary secretion.

Family:

GPCR

Sub Family:

Acetylcholine (Muscarinic)

Class:

Class A

Protein Name:

Uniprot Number:

P08912

Protein Aliases:

acetylcholine receptor, muscarinic 5

Gene Name:

CHRM5

Gene ID:

1133

Accession Number:

NM_001320917

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):

0.3

Ligand Concentration:

0.3 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

87nM - IC50

PubChem ID

174174

Name

Atropine

Measurement

0.34nM - IC50

PubChem ID

3014059

Name

4-Damp methiodide

Measurement

1.15nM - IC50

PubChem ID

44134815

Name

Methoctramine

Measurement

483nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

A muscarinic M5 subtype antagonist may reduce dopamine D1 central nervous stimulation and inhibit salivary secretion.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault