hERG - "High Throughput Pharmacology of hERG Channels on Nanion’s SyncroPatch 384PE"

icon sp96   SyncroPatch 384PE (a predecessor model of SyncroPatch 384i) application note   logo pdf   (0.6 MB)

Summary:

The hERG gene encodes a potassium channel responsible for the repolarization of the IKr current in cardiac cells. This channel is important in the repolarization of the cardiac action potential. Abnormalities in this channel can lead to long or short QT syndrome, leading to potentially fatal cardiac arrhythmia. Given the importance of this channel in maintaining cardiac function, and disturbances of channel activity by certain compounds such as antiarrhythmias and anti-psychotics, it has become an important target in compound safety screening. A large range of therapeutic agents with diverse chemical structures have been reported to induce long QT syndrome by inhibiting the hERG channel. These include antihistamines (e.g. Terfenadine), gastrointestinal prokinetic agents (e.g. Cisapride), amongst others. Therefore, it is important to test new therapeutics for actions on the hERG channel early on in the drug discovery process. Here we present high quality data with reliable pharmacology on hERG expressing CHO cells at a high throughput collected on the SyncroPatch 384PE. Current-voltage plots, and concentration response curves for the compounds pimozide, astemizole, cisapride and terfenadine are shown. The IC50 values for these compounds are within the expected range and success rates of 80% for completed experiments were recorded.

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