Voltage-gated ion channels (VGICs) and transient receptor potential (TRP) channels (VGIC and TRP channels)

Voltage-gated ion channels (VGICs) and transient receptor potential (TRP) channels represent two major superfamilies of transmembrane proteins essential for cellular excitability and sensory signaling. VGICs, which include sodium, potassium, and calcium channels, open or close in response to changes in the electrical potential across the cell membrane, facilitating the rapid propagation of action potentials in neurons and muscle cells (StatPearls, 2023; UniProt, 2024). TRP channels are primarily non-selective cation channels that function as cellular sensors for a vast array of stimuli, including temperature, pressure, and chemical ligands like capsaicin (Nature Reviews Drug Discovery, 2017; PMC, 2014). These channels are fundamental to physiological processes such as cardiac rhythmicity, neurotransmission, and the perception of pain and temperature. Mutations in the genes encoding these proteins lead to a variety of disorders known as channelopathies, such as Dravet syndrome, familial hemiplegic migraine, and various cardiac arrhythmias (StatPearls, 2023; IUPHAR/BPS, 2024). Consequently, they are major therapeutic targets for local anesthetics, anti-epileptics, anti-arrhythmics, and analgesics (Nature Reviews Drug Discovery, 2017; IUPHAR/BPS, 2024).

Other names

Voltage-sensitive ion channelsVGICsTRP channel superfamilyTransient receptor potential channel family

Drugs targeting these channels typically act as pore blockers, allosteric modulators, or gating modifiers to either inhibit or enhance ion conductance across the cell membrane (StatPearls, 2023; Nature Reviews Drug Discovery, 2017).