Valenzuela, C.; Delpón, E.; Franqueza, L.; Gay, P.; Pérez, O.; Tamargo, J.; Snyders, D.J. "Class III antiarrhythmic effects of zatebradine. Time-, state-, use-, and voltage-dependent block of hKv1.5 channels.". Circulation. 94(3): 562-570. (1996). (PMID: 8759103).
CONCLUSIONS These results indicate that (1) zatebradine is an open-channel blocker of hKv 1.5, (2) binding occurs in the internal mouth of the ion pore, (3) unbinding is required before the channel can close, and (4) zatebradine-induced block is use dependent because of slower recovery kinetics in the presence of the drug. These effects may explain the prolongation of the cardiac action potential and could be clinically relevant.
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