Key result
A radioactive rubidium (86Rb) efflux assay provides a high-throughput screening method to evaluate compound interactions with HERG K+ channels, with results affected by assay time and efflux rate.
The radioactive rubidium efflux assay provides a high-throughput method for evaluating compound interactions with HERG K+ channels, which is important for preclinical cardiac safety screening in the pharmaceutical industry.
May facilitate preclinical HERG screening; leaves open validation for clinical cardiac safety.
In this paper, we describe an assay using radioactive rubidium (86Rb) efflux to screen functional human ether-a go-go-related gene (HERG) K+ channels in a high-throughput screening (HTS) format. This assay offers an alternative way to examine junctional interactions between chemical compounds and HERG K+ channels. Follow-up experiments and discussions were carried out to address a variety of factors that affect potency evaluation within the Rb efflux assay. Factors that can affect the assay results, such as assay time, efflux rate, and compound blocking kinetics, are discussed in detail. Our results provide some explanations for the variances of the assay results and offer some guidelines for using the Rb efflux assay to evaluate compound interactions with HERG K+ channels in the pharmaceutical industry.
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Cheng et al. (2002) studied this question. Radioactive rubidium (86Rb) efflux assay was evaluated on Assay performance and factors affecting potency evaluation. A radioactive rubidium (86Rb) efflux assay provides a high-throughput screening method to evaluate compound interactions with HERG K+ channels, with results affected by assay time and efflux rate.
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