Validation of FLIPR Membrane Potential Dye for High Throughput Screening of Potassium Channel Modulators
2001; Elsevier BV; Volume: 6; Issue: 5 Linguagem: Inglês
10.1177/108705710100600504
ISSN2472-5560
AutoresKristi L. Whiteaker, Sujatha M. Gopalakrishnan, Duncan R. Groebe, Char‐Chang Shieh, Usha Warrior, David J. Burns, Michael J. Coghlan, Victoria Scott, Murali Gopalakrishnani,
Tópico(s)Analytical Chemistry and Sensors
ResumoA 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 K+ channel; K(ATP)) 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 K(ATP) 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.
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