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Target intelligence / Profile preview
Voltage-Gated Calcium Channel α2δ Subunit (CACNA2D)
- Target
- CACNA2D
- Molecular classification
- Ion channel subunit, Voltage-gated calcium channel subunit, Auxiliary subunit
01
Overview
The voltage-gated calcium channel α2δ subunit is an auxiliary protein of high-voltage-activated calcium channels (CaV1 and CaV2). It modulates channel trafficking, surface expression, and biophysical properties. There are four isoforms (α2δ-1 to α2δ-4), with α2δ-1 being the primary target of gabapentinoid drugs like gabapentin and pregabalin, used for neuropathic pain.
- Other names
- Calcium channel subunit alpha2deltaα2δ subunitCACNA2D1CACNA2D2CACNA2D3CACNA2D4
02
Mechanism of action
Binding to the α2δ subunit of voltage-gated calcium channels, primarily α2δ-1, to reduce calcium influx and neurotransmitter release.
03
Biological functions
Calcium channel modulationRegulation of channel traffickingRegulation of channel surface expressionSynaptogenesis
04
Disease associations
Neuropathic painEpilepsyAnxiety disordersFibromyalgia
05
Safety considerations
DizzinessSomnolencePeripheral edemaAbuse potential
06
Interacting drugs
Gabapentin
2 more in the full profile.
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