IndraLab

Statements


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"Inhibition of HERG potassium channels by domiphen bromide and didecyl dimethylammonium bromide."

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"Overall, we suspected that the HERG blockade by domiphen bromide and didecyl dimethylammonium bromide were mainly associated with the binding of the compounds to open channels."

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"First, both domiphen bromide and didecyl dimethylammonium bromide blocked HERG channel currents expressed in CHO cells in a voltage dependent and use dependent manner."

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"In summary, our results demonstrate that tetra-n-octylammonium bromide and benzethonium chloride inhibit HERG channel currents in the voltage dependent and use dependent manners."

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"Our data indicated that tetra-n-octylammonium bromide blocks HERG channels in both open and inactivated states (XREF_FIG), whereas benzethonium chloride preferentially blocks HERG channels in the open states."

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"The study of mechanism of HERG channel inhibition by tetra-n-octylammonium bromide and benzethonium chloride can provide additional insight of structure activity relationship of HERG channel inhibition and the molecular determinants of the interaction between the compounds and HERG channel proteins."

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"The use dependency of HERG channel blockade by 3 nM domiphen bromide and didecyl dimethylammonium bromide were examined with the voltage pulses shown in XREF_FIG."

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"Our data demonstrated that domiphen bromide and didecyl dimethylammonium bromide blocked the HERG channel with a preference for the activated channel state."

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"Domiphen bromide and didecyl dimethylammonium bromide inhibited HERG channel currents in a dose dependent manner with IC 50 values of 9 nM and 5 nM, respectively."

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"The result indicates that tetra-n-octylammonium bromide blocks HERG channels in a use dependent manner."

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"In the present study, the potential mechanisms for HERG channel inhibition by tetra-n-octylammonium bromide and benzethonium chloride, two most potent HERG channel inhibitors found among the QACs examined, were studied using whole-cell patch clamp experiments in a CHO cell line stably expressing HERG channels."

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"The results indicate that domiphen bromide blocks HERG channels in a use dependent manner."

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"Concentration dependent inhibition of HERG channel by tetra-n-octylammonium bromide and benzethonium chloride."

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"The properties of HERG channel inhibition by tetra-n-octylammonium bromide and benzethonium chloride are highly similar to verapamil and cisapride (XREF_TABLE)."

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"In addition, the domiphen bromide and didecyl dimethylammonium bromide inhibition of heterologously expressed HERG channels was voltage sensitive, increasing for steps more depolarized than -40 mV and reaching a maximum at approximately 0 mV (XREF_FIG)."

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"In consistent with the " crossover " phenomenon, tetra-n-octylammonium bromide slowed the deactivation rate of HERG channel tail current (XREF_FIG)."

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"Use dependent inhibition of HERG channels by tetra-n-octylammonium bromide and benzethonium chloride."

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"In this study, we found that benzethonium chloride, domiphen bromide, and tetra-n-octylammonium bromide significantly inhibited hERG channel activity in both the thallium influx assay and the patch clamp experiment."