Target intelligence / Profile preview

Voltage-Gated Sodium Channel (Neuronal) (VGSC)

Target
VGSC
Molecular classification
Ion channel, Voltage-gated ion channel
01

Overview

Voltage-gated sodium channels (VGSCs) are transmembrane proteins responsible for the rapid influx of sodium ions into excitable cells, such as neurons, in response to changes in membrane potential. This process is essential for the initiation and propagation of action potentials. The core functional unit is the alpha subunit, composed of four homologous domains (I–IV), each containing six transmembrane segments (S1–S6). The S4 segment acts as the voltage sensor, and the P-loops between S5 and S6 segments form the ion-selective pore. VGSCs are major drug targets, with local anesthetics and antiepileptics blocking these channels.

Other names
Sodium channelNav1.1Nav1.2Nav1.3Nav1.6SCN1ASCN2ASCN3ASCN8A
02

Mechanism of action

Channel blockers that prevent sodium ion influx, stabilizing inactive states of the channel and/or accessing binding sites within the pore during depolarization events.

03

Biological functions

Action potential initiationAction potential propagationNeuronal excitabilityElectrical signaling
04

Disease associations

EpilepsyNeuropathic painAtaxiaPeriodic paralysisMultiple sclerosisBrain tumors
05

Safety considerations

Potential for off-target effects due to isoform diversityArrhythmias
06

Interacting drugs

Local anesthetics

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