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:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

10 min at 37°C

Control Inhibitor:

PD 102807

Control Activator:

acetylcholine (100 nM)

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 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

4848

Name

Pirenzepine

Measurement

550nM - IC50

PubChem ID

3014059

Name

4-Damp methiodide

Measurement

9.8nM - IC50

PubChem ID

4995951

Name

PD 102807

Measurement

280nM - IC50

PubChem ID

Name

AF-DX 116

Measurement

7300nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

A muscarinic M4 subtype antgonist may facilitate dopamine D1 central nervous system stimulation.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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