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Issue 13, 2012
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Ion channel drug potency assay with an artificial bilayer chip

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Abstract

The potency of pharmaceutical compounds acting on ion channels can be determined through measurements of ion channel conductance as a function of compound concentration. We have developed an artificial lipid bilayer chip for simple, fast, and high-yield measurement of ion channel conductance with simultaneous solution perfusion. Here we show the application of this chip to the measurement of the mammalian cold and menthol receptor TRPM8. Ensemble measurements of TRPM8 as a function of concentration of menthol and 2-aminoethoxydiphenyl borate (2-APB) enabled efficient determination of menthol's EC50 (111.8 μM ± 2.4 μM) and 2-APB's IC50 (4.9 μM ± 0.2 μM) in agreement with published values. This validation, coupled with the compatibility of this platform with automation and parallelization, indicates significant potential for large-scale pharmaceutical ion channel screening.

Graphical abstract: Ion channel drug potency assay with an artificial bilayer chip

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Publication details

The article was received on 23 Jan 2012, accepted on 30 Mar 2012 and first published on 30 Mar 2012


Article type: Paper
DOI: 10.1039/C2LC40087A
Citation: Lab Chip, 2012,12, 2409-2413
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    Ion channel drug potency assay with an artificial bilayer chip

    A. M. El-Arabi, C. S. Salazar and J. J. Schmidt, Lab Chip, 2012, 12, 2409
    DOI: 10.1039/C2LC40087A

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