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Target intelligence / Profile preview
Voltage-gated sodium channel Nav1.8 (Nav1.8)
- Target
- Nav1.8
- Molecular classification
- Ion channel, Voltage-gated ion channel, Sodium channel
01
Overview
Nav1.8 is a tetrodotoxin-resistant voltage-gated sodium channel primarily expressed in sensory neurons, particularly DRG neurons. It plays a major role in pain perception, especially in chronic inflammatory and neuropathic pain states, as well as cold pain sensation. Gain-of-function mutations are associated with increased pain sensitivity, and variants have been linked to multiple sclerosis and cardiac rhythm disorders. Selective inhibitors are under development as analgesics.
- Other names
- SNSSensory neuron-specific sodium channelSCN10A
02
Mechanism of action
Selective Nav1.8 inhibition
03
Biological functions
Action potential generationNociceptionPain signalingCold pain sensation
04
Disease associations
Neuropathic painInflammatory painChronic painCold-induced painMultiple sclerosisCardiac arrhythmias
05
Safety considerations
Potential for off-target effects on other voltage-gated sodium channelsCardiac effects due to expression in cardiac innervation
06
Interacting drugs
A-803467
2 more in the full profile.
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