Key result
Imipramine and astemizole inhibit hEag1 K+ channels by crossing the membrane in uncharged form and selectively binding to open channels from the intracellular side in their charged forms.
Imipramine and astemizole block hEag1 potassium channels from the intracellular side, providing mechanistic insights into their effects on channel function.
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Imipramine and astemizole block hEag1 at distinct sites; leaves open selective targeting for cancer therapy.
García-Ferreiro et al. (2004) studied Cancer cell lines / hEag1 K+ channels. Imipramine and astemizole was evaluated on Mechanism of hEag1 channel block. Imipramine and astemizole inhibit hEag1 K+ channels by crossing the membrane in uncharged form and selectively binding to open channels from the intracellular side in their charged forms.
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