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:

M3

Uniprot Number:

P20309

Protein Aliases:

acetylcholine receptor, muscarinic 3

Gene Name:

CHRM3

Gene ID:

1131

Accession Number:

NM_000740

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

Acetylcholine

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 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

PubChem ID

24277861

Name

Oxotremorine

Measurement

19.21nM - EC50

PubChem ID

24277829

Name

Carbachol

Measurement

57.08nM - EC50

PubChem ID

57653883

Name

Acetylcholine

Measurement

5.2nM - EC50

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

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