E-4031

E-4031
Clinical data
Other names(1-[2-(6-methyl-2-pyridyl)ethyl]-4-(4-methylsulfonyl-aminobenzoyl)piperidine)
Identifiers
  • N-[4-[1-[2-(6-Methylpyridin-2-yl)ethyl]piperidine-4-carbonyl]phenyl]
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H27N3O3S
Molar mass401.53 g·mol−1
3D model (JSmol)
  • Cc1cccc(n1)CCN2CCC(CC2)C(=O)c3ccc(cc3)NS(=O)(=O)C
  • InChI=1S/C21H27N3O3S/c1-16-4-3-5-19(22-16)12-15-24-13-10-18(11-14-24)21(25)17-6-8-20(9-7-17)23-28(2,26)27/h3-9,18,23H,10-15H2,1-2H3
  • Key:SRUISGSHWFJION-UHFFFAOYSA-N
  (verify)

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

Chemistry

E-4031 is a synthesized toxin that is a methanesulfonanilide class III antiarrhythmic drug.

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. The hERG channel is encoded by ether-a-go-go related gene (hERG).

Mode of action

E-4031 blocks hERG-type potassium channels by binding to the open channels. 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.

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

Toxicity

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

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.


This page was last updated at 2024-01-14 07:59 UTC. Update now. View original page.

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