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Validation of FLIPR Membrane Potential Dye for High Throughput Screening of Potassium Channel Modulators

Neuroscience Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Sujatha M. Gopalakrishnan

Advanced Technology, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Duncan Groebe

Advanced Technology, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Char-Chang Shieh

Neuroscience Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Usha Warrior

Advanced Technology, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

David J. Burns

Advanced Technology, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Michael J. Coghlan

Neuroscience Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Victoria E. Scott

Neuroscience Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

Murali Gopalakrishnani

Neuroscience Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL

A fluorescence-based assay using the FLIPR Membrane Potential Assay Kit (FMP) was evaluated for functional characterization and high throughput screening (HTS) of potassium channel (ATP-sensitive Ki channel; KATP) modulators. The FMP dye permits a more sensitive evaluation of changes in membrane potential with a more rapid response time relative to DiBAC₄(3). The time course of responses is comparable to ligand-evoked activation of the channel measured by patch-clamp studies. The pharmacological profile of the K+ channel evaluated by using reference KATP channel openers is in good agreement with that derived previously by DiBAC₄(3)-based FLIPR assays. Improved sensitivity of responses together with the diminished susceptibility to artifacts such as those evoked by fluorescent compounds or quenching agents makes the FMP dye an alternative choice for HTS screening of potassium channel modulators.

Journal of Biomolecular Screening, Vol. 6, No. 5, 305-312 (2001)
DOI: 10.1177/108705710100600504


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