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Target intelligence / Profile preview
High-voltage activated calcium channels (HVA calcium channels)
- Target
- HVA calcium channels
- Molecular classification
- Calcium channel family, HVA calcium channel family, Multi-subunit protein complex, Voltage-gated ion channels
01
Overview
High-voltage activated calcium channels are essential multi-subunit membrane proteins that open in response to membrane depolarization, allowing calcium ions to enter cells along their electrochemical gradient. They are widely distributed and play crucial roles in cellular signaling and various physiological processes. Structurally, they consist of a pore-forming α₁ subunit, which contains the voltage-sensing machinery and drug/toxin-binding sites, and auxiliary subunits (α₂δ, β, γ). HVA channels require stronger depolarization to open compared to LVA channels. Subtypes include L-type (Cav1), P/Q-type (Cav2.1), N-type (Cav2.2), and R-type (Cav2.3), each with distinct properties and roles.
02
Mechanism of action
Drugs targeting HVA calcium channels primarily act as blockers or antagonists, preventing the influx of calcium ions into cells upon channel opening.
03
Biological functions
Excitation-contraction couplingNeurotransmitter releaseGene expression regulationSynaptic plasticityNeuronal excitabilityHormone secretion
04
Disease associations
PainNeurodegenerative diseases (Alzheimer's, Parkinson's)Multiple sclerosisEpilepsyHypertension
05
Safety considerations
Peripheral side effects (especially for CNS-specific antagonists)
06
Interacting drugs
Dihydropyridines
5 more in the full profile.
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