nAChR (alpha4/beta2) Human Ion Channel Binding Agonist Radioligand LeadHunter Assay - FR

Item: 3029

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Subtypes of α4-nicotinic acetylcholine (nACh) receptors are considered to occur naturally while recombinant α4β2 receptors are the most abundant high affinity binding sites in the brain. Nicotinic acetylcholine α4β-nACh, cytisine receptor agonism may improve learning and memory, increase dopaminergic transmission and exhibit analgesic activity. Receptors antagonists may find use as tobacco smoking cessation agents.

Family:

Ion Channel

Sub Family:

Acetylcholine (Nicotinic)

Class:

Ligand-Gated

Protein Name:

nAChR

Uniprot Number:

P43681

Protein Aliases:

acetylcholine receptor, nicotinic, alpha 4 (neuronal)

Gene Name:

CHRNA4

Gene ID:

1137

Gene Aliases:

BFNC

Accession Number:

XM_017027624

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]cytisine

Ligand Kd (nM):

0.3

Ligand Concentration:

0.6 nM

Non Specific:

10 µM Nicotine

Incubation:

120 min at 4°C

Control Inhibitor:

nicotine

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:

15 Business Days

Reference Compound Data

PubChem ID

5831

Name

Carbachol

Measurement

370nM - IC50

PubChem ID

57653815

Name

Atropine sulfate salt

Measurement

- IC50

PubChem ID

11957628

Name

nicotine

Measurement

5.9nM - IC50

PubChem ID

90488742

Name

alpha bungarotoxin

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Nicotinic acetylcholine a4b-nACh, cytisine receptor agonism may improve learning and memory, increase dopaminergic transmission and exhibit analgesic activity. Receptors antagonists may find use as tobacco smoking cessation agents.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault