ion channel electrophysiology | hERG potassium ion | potassium sodium calcium ion | cardiomyocytes
In cardiomyocytes, the human Ether-a-go-go mediates a delayed rectifier potassium current (IKr) Related a potassium channel encoded by Gene (hERG), and IKr inhibition is the most important mechanism of drug-induced QT interval prolongation. Because of its special molecular structure, hERG can be inhibited by various compounds. At present, testing the effect of compounds on hERG potassium channels is a key step in preclinical evaluation of the cardiac safety of compounds, and is also the necessary information for approval of new drugs required by FDA. The hERG gene plays an important role in the physiological process. The potassium channel expressed by hERG has the property of inward rectification, and the inward Ikr is open in all phases of the action potential of myocardial cells, and the conductance is the largest in the 3 phase of the action potential repolarization and the resting potential. It shows obvious inward current when it is hyperpolarized, and outward current when it is slightly depolarized, so as to maintain the stability of the resting potential. The hERG potassium channel is rapidly activated when the action potential is depolarised to about -30mV and persists until the end of the phase 3 action potential. Thus, hHERG potassium channels can regulate the propagation of premature contractions due to the early arrival of excitatory impulses from the myocardial sinoatrial node or heterologous sources.
Technical principle
| Detect dimension | ||
|---|---|---|
| myocardial cell | Basic indicators | action potential |
| Detection of basic parameters of cell electrophysiology | ||
| potassium ion | channel current | potassium channel current |
| state detection | active state | inactive state | |
| hERG Potassium Channel Specific Assay | ||
| sodium ion | channel current | sodium ion channel current |
| state detection | active state | inactive state | |
| Voltage-gated sodium channel detection | ||
| calcium ion | channel current | calcium channel current |
| state detection | active state | inactive state | |
| L-type calcium channel specific analysis | ||
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