Molecular Determinants for the High-Affinity Blockade of Human Ether-à-go-go-Related Gene K+ Channel by Tolterodine

In conclusion, tolterodine is an open-state blocker of hERG K+ channel with nanomolar potency. Y652 and F656, 2 aromatic residues on the inner S6 helix, are responsible for the high-affinity binding of tolterodine to hERG channel.
Source: Journal of Cardiovascular Pharmacology - Category: Cardiology Tags: Original Article Source Type: research