Key result
A cell-based fluorescent screening assay using HL-1 cells successfully identified analogues of amiloride and propafenone as GIRK1/4 channel blockers at concentrations <1 µM (Z' factor 0.5-0.6).
Population
Mouse atrial HL-1 cell line expressing the GIRK1/4 channel
Comparison
Small compound library of Na and K channel… vs Control solution
Design
Preclinical
Authors
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May accelerate GIRK1/4 blocker discovery for AF; leaves open translation to clinical efficacy and safety.
Effect estimate: Z' factor = 0.5-0.6
A newly developed cell-based fluorescent screening assay successfully identifies GIRK1/4 channel blockers, providing a tool for discovering novel atrial fibrillation therapies.
Kenneth B. Walsh (2010) studied Atrial fibrillation. Small compound library of Na(+) and K(+) channel modulators vs. Control solution was evaluated on Fluorescent signal indicative of K(+) efflux through the GIRK1/4 channel (Z' factor = 0.5-0.6). A cell-based fluorescent screening assay using HL-1 cells successfully identified analogues of amiloride and propafenone as GIRK1/4 channel blockers at concentrations <1 µM (Z' factor 0.5-0.6).
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