Key result
Flecainide produced a concentration-dependent blockade of total integrated current flow (IC50 ~10 microM) in Kv4.3/KChIP2 channels coassembled with MiRP1 and/or DPP6 beta-subunits.
Population
Chinese hamster ovary cells stably expressing K4.3/KChIP2 channels, and transiently transfected with either…
Comparison
Flecainide (0.1-100 microM) vs Control conditions (no flecainide)
Design
Preclinical
Authors
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May modulate Ito in experimental models; leaves open clinical relevance for arrhythmia therapy.
Effect estimate: IC50 approximately 10 microM
Flecainide directly binds to the Kv4.3 alpha-subunit in open and inactivated states, with beta-subunits modulating the blockade by altering gating function.
Radicke et al. (2008) studied this question. Flecainide vs. control conditions was evaluated on blockade of total integrated current flow (IC50 approximately 10 microM). Flecainide produced a concentration-dependent blockade of total integrated current flow (IC50 ~10 microM) in Kv4.3/KChIP2 channels coassembled with MiRP1 and/or DPP6 beta-subunits.
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