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E-4031

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E-4031

E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.[1]

Chemistry

E-4031 is a synthetized toxin that is a methanesulfonanilide class III antiarrhythmic drug.[2]

Target

E-4031 acts on a specific class of voltage-gated potassium channels mainly found in the heart, the hERG channels. hERG channels (Kv11.1) mediate the IKr current, which repolarizes the myocardial cells.[3][4] The hERG channel is encoded by ether-a-go-go related gene (hERG).[5]

Mode of action

E-4031 blocks hERG-type potassium channels [5][6] by binding to the open channels.[7] Its structural target within the hERG-channel is unclear, but some other methanesulfonanilide class III antiarrhythmic drugs are known to bind to the S6 domain or C-terminal of the hERG-channel.[8][9][10][11][12][13]

Reducing IKr in myocardial cells prolongs the cardiac action potential and thus prolongs the QT-interval.[7][14] In non-cardiac cells, blocking Ikr has a different effect: it increases the frequency of action potentials.[5]

Toxicity

As E-4031 can prolong the QT-interval, it can cause lethal arrhythmias.[13]

Therapeutic use

E-4031 is solely used for research purposes. So far, one clinical trial has been conducted to test the effect of E-4031 on prolongation of the QT-interval.[15]

References

  1. REDIRECT
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