Why the study?
The mechanism of block and slow recovery from block of HERG channels by methanesulfonanilide class III antiarrhythmic agents like MK-499 was not fully understood.
MK-499 blocks HERG channels by binding to a site within the inner vestibule that is accessed from the cytoplasm only after channel opening, trapping the drug when the activation gate closes.
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Mitcheson et al. (2000) conducted a review in HERG potassium channel block. MK-499 vs. Wild-type HERG channels or pre-drug baseline was evaluated on IC50 for channel block.
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