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Target intelligence / Profile preview
Hyperpolarization-activated cyclic nucleotide–gated channel (HCN channel)
- Target
- HCN channel
- Molecular classification
- Ion channel, Voltage-gated ion channel
01
Overview
HCN channels are nonselective voltage-gated cation channels that are activated by membrane hyperpolarization. They are tetrameric proteins composed of four subunits (HCN1-4) and are primarily found in the heart and brain. HCN channels generate the pacemaker current (I_f/I_h), which is crucial for regulating cardiac and neuronal rhythmicity. Dysfunction of HCN channels has been implicated in cardiac arrhythmias and epilepsy. The drug ivabradine selectively targets cardiac-specific HCN isoforms to reduce heart rate.
02
Mechanism of action
Selective inhibition of HCN channels
03
Biological functions
Pacemaker current generationRegulation of neuronal rhythmicityMaintenance of resting membrane potentialDendritic integrationSynaptic transmissionCardiac pacemaking
04
Disease associations
Cardiac arrhythmiasEpilepsy
05
Safety considerations
Potential for cardiac side effects due to altered heart rateNeurological side effects
06
Interacting drugs
Ivabradine
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