Target intelligence / Profile preview

Voltage-gated potassium channel (Delayed rectifier) (Kv channel (Delayed rectifier))

Target
Kv channel (Delayed rectifier)
Molecular classification
Ion channel, Voltage-gated ion channel
01

Overview

The delayed rectifier potassium current (IK) is a fundamental voltage-gated current responsible for the repolarization phase of action potentials in excitable cells, including NG108-15 neuroblastoma x glioma hybrid cells and cerebellar granule neurons. In these specific cell types, the current is primarily mediated by channels from the Kv2 (notably Kv2.1/KCNB1) and Kv3 (notably Kv3.1/KCNC1) families, which open with a characteristic delay following membrane depolarization. This delayed activation allows the initial sodium influx to trigger an action potential before the potassium efflux returns the membrane to its resting potential. Dysregulation of these channels is linked to various neurological disorders, such as epilepsy and ataxia, due to their critical role in controlling neuronal firing frequency and excitability. Pharmacological modulation of IK using blockers like tetraethylammonium or specific Kv channel modulators represents a strategy for treating hyperexcitability disorders.

Other names
Delayed rectifier potassium currentIKVoltage-gated potassium channel subfamily B member 1Kv2.1Voltage-gated potassium channel subfamily C member 1Kv3.1
02

Mechanism of action

Modulation of potassium ion efflux through the channel pore to regulate membrane potential and cellular excitability.

03

Biological functions

Repolarization of action potentialsRegulation of neuronal excitabilityMaintenance of resting membrane potentialControl of neuronal firing frequency
04

Disease associations

EpilepsyAtaxiaNeurodegenerative diseaseSeizure disordersSchizophrenia
05

Safety considerations

Risk of seizuresCardiac arrhythmias (off-target effects on hERG)Neuromuscular dysfunctionCognitive impairment
06

Interacting drugs

Tetraethylammonium

4 more in the full profile.

07

Biomarkers

KCNB1 expression levelsKCNC1 expression levelsElectrophysiological current density (patch-clamp)

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