A channel modulator, or ion channel modulator, is a type of drug which modulates ion channels. They include channel blockers and channel openers.
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
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
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TRPA |
Activators |
- 4-Hydroxynonenal
- 4-Oxo-2-nonenal
- 4,5-EET
- 12S-HpETE
- 15-Deoxy-Δ12,14-prostaglandin J2
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α-Sanshool (ginger, Sichuan and melegueta peppers)
- Acrolein
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Allicin (garlic)
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Allyl isothiocyanate (mustard, radish, horseradish, wasabi)
- AM404
- ASP-7663
- Bradykinin
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Cannabichromene (cannabis)
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Cannabidiol (cannabis)
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Cannabigerol (cannabis)
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Cinnamaldehyde (cinnamon)
- CR gas (dibenzoxazepine; DBO)
- CS gas (2-chlorobenzal malononitrile)
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Cuminaldehyde (cumin)
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Curcumin (turmeric)
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Dehydroligustilide (celery)
- Diallyl disulfide
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Dicentrine (Lindera spp.)
- Farnesyl thiosalicylic acid
- Formalin
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Gingerols (ginger)
- Hepoxilin A3
- Hepoxilin B3
- Hydrogen peroxide
- Icilin
- Isothiocyanate
- JT-010
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Ligustilide (celery, Angelica acutiloba)
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Linalool (Sichuan pepper, thyme)
- Methylglyoxal
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Methyl salicylate (wintergreen)
- N-Methylmaleimide
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Nicotine (tobacco)
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Oleocanthal (olive oil)
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Paclitaxel (Pacific yew)
- Paracetamol (acetaminophen)
- PF-4840154
- Phenacyl chloride
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Polygodial (Dorrigo pepper)
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Shogaols (ginger, Sichuan and melegueta peppers)
- Tear gases
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Tetrahydrocannabinol (cannabis)
- Tetrahydrocannabiorcol
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Thiopropanal S-oxide (onion)
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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
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α-Sanshool (ginger, Sichuan and melegueta peppers)
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Allicin (garlic)
- AM404
- Anandamide
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Bisandrographolide (Andrographis paniculata)
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Camphor (camphor laurel, rosemary, camphorweed, African blue basil, camphor basil)
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Cannabidiol (cannabis)
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Cannabidivarin (cannabis)
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Capsaicin (chili pepper)
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Carvacrol (oregano, thyme, pepperwort, wild bergamot, others)
- DHEA
- Diacyl glycerol
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Dihydrocapsaicin (chili pepper)
- Estradiol
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Eugenol (basil, clove)
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Evodiamine (Euodia ruticarpa)
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Gingerols (ginger)
- GSK1016790A
- Heat
- Hepoxilin A3
- Hepoxilin B3
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Homocapsaicin (chili pepper)
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Homodihydrocapsaicin (chili pepper)
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Incensole (incense)
- Lysophosphatidic acid
- Low pH (acidic conditions)
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Menthol (mint)
- N-Arachidonoyl dopamine
- N-Oleoyldopamine
- N-Oleoylethanolamide
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Nonivamide (PAVA) (PAVA spray)
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Nordihydrocapsaicin (chili pepper)
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Paclitaxel (Pacific yew)
- Paracetamol (acetaminophen)
- Phenylacetylrinvanil
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Phorbol esters (e.g., 4α-PDD)
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Piperine (black pepper, long pepper)
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Polygodial (Dorrigo pepper)
- Probenecid
- Protons
- RhTx
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Rutamarin (Ruta graveolens)
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Resiniferatoxin (RTX) (Euphorbia resinifera/pooissonii)
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Shogaols (ginger, Sichuan and melegueta peppers)
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Tetrahydrocannabivarin (cannabis)
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Thymol (thyme, oregano)
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Tinyatoxin (Euphorbia resinifera/pooissonii)
- Tramadol
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Vanillin (vanilla)
- Zucapsaicin
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Blockers |
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