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
- ^ 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.
Types | - ♦ Miscellaneous: Precursor
- Cofactor
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Classes | Enzyme | see Enzyme inhibition |
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Ion channel | See Ion channel modulators |
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Receptor & transporter | |
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Miscellaneous | - Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
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Ion channel modulators |
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Calcium | VDCCsTooltip Voltage-dependent calcium channels | |
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Potassium | VGKCsTooltip Voltage-gated potassium channels | |
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IRKsTooltip Inwardly rectifying potassium channel | Blockers | |
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Activators | - GIRKTooltip G protein-coupled inwardly rectifying potassium channel-specific: ML-297 (VU0456810)
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KCaTooltip Calcium-activated potassium channel | |
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K2PsTooltip Tandem pore domain potassium channel | |
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Sodium | VGSCsTooltip Voltage-gated sodium channels | |
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ENaCTooltip Epithelial sodium channel | |
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ASICsTooltip Acid-sensing ion channel | |
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Chloride | CaCCsTooltip Calcium-activated chloride channel | |
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CFTRTooltip Cystic fibrosis transmembrane conductance regulator | |
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Unsorted | |
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Others | TRPsTooltip Transient receptor potential channels | |
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LGICsTooltip Ligand gated ion channels | |
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See also: Receptor/signaling modulators • Transient receptor potential channel modulators |
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TRPA | Activators | - 4-Hydroxynonenal
- 4-Oxo-2-nonenal
- 4,5-EET
- 12S-HpETE
- 15-Deoxy-Δ12,14-prostaglandin J2
- α-Sanshool (ginger, Sichuan and melegueta peppers)
- Acrolein
- Allicin (garlic)
- Allyl isothiocyanate (mustard, radish, horseradish, wasabi)
- AM404
- ASP-7663
- Bradykinin
- Cannabichromene (cannabis)
- Cannabidiol (cannabis)
- Cannabigerol (cannabis)
- Cinnamaldehyde (cinnamon)
- CR gas (dibenzoxazepine; DBO)
- CS gas (2-chlorobenzal malononitrile)
- Cuminaldehyde (cumin)
- Curcumin (turmeric)
- Dehydroligustilide (celery)
- Diallyl disulfide
- Dicentrine (Lindera spp.)
- Farnesyl thiosalicylic acid
- Formalin
- Gingerols (ginger)
- Hepoxilin A3
- Hepoxilin B3
- Hydrogen peroxide
- Icilin
- Isothiocyanate
- JT-010
- Ligustilide (celery, Angelica acutiloba)
- Linalool (Sichuan pepper, thyme)
- Methylglyoxal
- Methyl salicylate (wintergreen)
- N-Methylmaleimide
- Nicotine (tobacco)
- Oleocanthal (olive oil)
- Paclitaxel (Pacific yew)
- Paracetamol (acetaminophen)
- PF-4840154
- Phenacyl chloride
- Polygodial (Dorrigo pepper)
- Shogaols (ginger, Sichuan and melegueta peppers)
- Tear gases
- Tetrahydrocannabinol (cannabis)
- Tetrahydrocannabiorcol
- Thiopropanal S-oxide (onion)
- Umbellulone (Umbellularia californica)
- WIN 55,212-2
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Blockers | |
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TRPC | |
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TRPM | |
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TRPML | |
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TRPP | |
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TRPV | Activators | - 2-APB
- 5',6'-EET
- 9-HODE
- 9-oxoODE
- 12S-HETE
- 12S-HpETE
- 13-HODE
- 13-oxoODE
- 20-HETE
- α-Sanshool (ginger, Sichuan and melegueta peppers)
- Allicin (garlic)
- AM404
- Anandamide
- Bisandrographolide (Andrographis paniculata)
- Camphor (camphor laurel, rosemary, camphorweed, African blue basil, camphor basil)
- Cannabidiol (cannabis)
- Cannabidivarin (cannabis)
- Capsaicin (chili pepper)
- Carvacrol (oregano, thyme, pepperwort, wild bergamot, others)
- DHEA
- Diacyl glycerol
- Dihydrocapsaicin (chili pepper)
- Estradiol
- Eugenol (basil, clove)
- Evodiamine (Euodia ruticarpa)
- Gingerols (ginger)
- GSK1016790A
- Heat
- Hepoxilin A3
- Hepoxilin B3
- Homocapsaicin (chili pepper)
- Homodihydrocapsaicin (chili pepper)
- Incensole (incense)
- Lysophosphatidic acid
- Low pH (acidic conditions)
- Menthol (mint)
- N-Arachidonoyl dopamine
- N-Oleoyldopamine
- N-Oleoylethanolamide
- Nonivamide (PAVA) (PAVA spray)
- Nordihydrocapsaicin (chili pepper)
- Paclitaxel (Pacific yew)
- Paracetamol (acetaminophen)
- Phenylacetylrinvanil
- Phorbol esters (e.g., 4α-PDD)
- Piperine (black pepper, long pepper)
- Polygodial (Dorrigo pepper)
- Probenecid
- Protons
- RhTx
- Rutamarin (Ruta graveolens)
- Resiniferatoxin (RTX) (Euphorbia resinifera/pooissonii)
- Shogaols (ginger, Sichuan and melegueta peppers)
- Tetrahydrocannabivarin (cannabis)
- Thymol (thyme, oregano)
- Tinyatoxin (Euphorbia resinifera/pooissonii)
- Tramadol
- Vanillin (vanilla)
- Zucapsaicin
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Blockers | |
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See also: Receptor/signaling modulators • Ion channel modulators |
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