nAChR (α4β2) Functional Antagonist Assay Service

Nicotinic acetylcholine receptor (nAChR) α4β2 Functional Cell-based Antagonist Assay for compound screening and profiling via fluorescence-based quantification of intracellular calcium.

Target Overview
CAT#

nAChR α4β2 Functional Antagonist

Synonyms

CHRNA4/CHRNB2, Alpha-4 beta-2 nicotinic receptor

GPCR Target

Human nAChR (α4β2)

Cell Line

CHO-K1/OPRM1/Gα15

Scientific Information

ACHA4 (https://www.uniprot.org/uniprotkb/P43681/entry)
ACHB2 (https://www.uniprot.org/uniprotkb/P17787/entry)

Assay Properties
Protocol

30 min incubation with antagonist; nAChR α4β2 activation by agonist application using FLIPR Penta system cells treated with Calcium 6 dye; fluorescence kinetic measurement

Readout

Calcium 6 dye fluorescence tracking changes in intracellular calcium

Reference Compound IC50
Compound IC50 (nM) Agonist (nM)
Mepyramine (21) Epibatidine (300)
Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website In Vitro Safety Pharmacology Profiling

Reference compound inhibition of nAChR α4β2

Reference compound inhibition of nAChR α4β2