Channel modulator

Type of drug which modulates ion channels

A channel modulator, or ion channel modulator, is a type of drug which modulates ion channels. They include channel blockers and channel openers.[1]

Direct modulators

Ion channels are typically categorised by gating mechanism and by the ion they conduct. Note that an ion channel may overlap between different categories. Some channels conduct multiple ion currents and some are gated by multiple mechanisms.

Examples of targets for modulators include:

Voltage-gated ion channels

  • Calcium channel: see also Calcium channel blocker, Calcium channel opener
  • Potassium channel: see also Potassium channel blocker, Potassium channel opener
  • Sodium channel: see also Sodium channel blocker, Sodium channel opener
  • Chloride channel: see also Chloride channel blocker, Chloride channel opener
  • Transient receptor potential channel


Ligand gated ion channels

Ion channels gated by other mechanisms (e.g. light gated and mechanosensitive ion channels). These types of channels can also be pharmacologically modulated. For lists of the substances that pharmacologically modulate them, see their respective articles.

Indirect modulators

Ion channels can also be modulated indirectly. For example with G protein coupled receptors (GPCRs), for G protein coupled inward rectifier potassium channels (GIRKs) and M channels. Ion channels can also be modulated by reuptake inhibitors and releasing agents.

See also

References

  1. ^ Birch, PJ; Dekker, LV; James, IF; Southan, A; Cronk, D (1 May 2004). "Strategies to identify ion channel modulators: current and novel approaches to target neuropathic pain". Drug Discovery Today. 9 (9): 410–8. doi:10.1016/S1359-6446(04)03043-0. PMID 15081958.
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TypesClasses
Enzyme
see Enzyme inhibition
Ion channel
See Ion channel modulators
Receptor &
transporter
BA/M
Adrenergic
Dopaminergic
Histaminergic
Serotonergic
AA
GABAergic
Glutamatergic
Cholinergic
Cannabinoidergic
Opioidergic
Other
Miscellaneous
  • Cofactor (see Enzyme cofactors)
  • Precursor (see Amino acids)
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Ion channel modulators
Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
  • GIRKTooltip G protein-coupled inwardly rectifying potassium channel-specific: ML-297 (VU0456810)
KCaTooltip Calcium-activated potassium channel
Blockers
  • BKCa-specific: Ethanol (alcohol)
  • GAL-021
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
  • Solnatide
ASICsTooltip Acid-sensing ion channel
Blockers
Chloride
CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
  • See here instead.
LGICsTooltip Ligand gated ion channels
  • See here instead.
See also: Receptor/signaling modulators • Transient receptor potential channel modulators
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TRP channel modulators
TRPA
Activators
Blockers
TRPC
Activators
Blockers
TRPM
Activators
Blockers
TRPML
Activators
Blockers
TRPP
Activators
Blockers
TRPV
Activators
Blockers
See also: Receptor/signaling modulators • Ion channel modulators


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