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Target intelligence / Profile preview
Acetylcholine-Regulated Inwardly Rectifying Potassium Channel (I_KACh)
- Target
- I_KACh
- Molecular classification
- Ion channel, Potassium channel, G protein-coupled inwardly rectifying potassium channel (GIRK)
01
Overview
The acetylcholine-regulated inwardly rectifying potassium channel mediates key parasympathetic effects on cardiac rhythm through direct activation via muscarinic receptors. Its dysregulation contributes importantly to atrial fibrillation pathophysiology. Pharmacologic inhibition represents a promising avenue for developing safer antiarrhythmic therapies focused on atria-specific targets.
- Other names
- Acetylcholine-gated K+ channelMuscarinic K+ channelGIRK4/Kir3.4Acetylcholine-activated potassium channel
02
Mechanism of action
Activation by G protein βγ subunits released upon acetylcholine binding to muscarinic M2 receptors, leading to increased potassium permeability and hyperpolarization.
03
Biological functions
Regulation of membrane potentialRegulation of heart rateParasympathetic signaling
04
Disease associations
Atrial fibrillationArrhythmiaSleep-disordered breathing-related AF
05
Safety considerations
Potential for ventricular proarrhythmic effects (less than other antiarrhythmics)
06
Interacting drugs
XAF-1407
2 more in the full profile.
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