A-967079 |
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(1E,3E)-1-(4-fluorophenyl)-2-methyl-1-penten-3-one oxime
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| Formula | C12H14FNO |
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| Molar mass | 207.248 g·mol−1 |
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CC/C(=N/O)/C(=C/C1=CC=C(C=C1)F)/C
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InChI=1S/C12H14FNO/c1-3-12(14-15)9(2)8-10-4-6-11(13)7-5-10/h4-8,15H,3H2,1-2H3/b9-8+,14-12- Key:HKROEBDHHKMNBZ-BYKJOZEVSA-N
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A-967079 is a drug which acts as a potent and selective antagonist for the TRPA1 receptor. It has analgesic and antiinflammatory effects and is used in scientific research, but has not been developed for medical use.[1][2][3][4][5]
References
- ^ Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, et al. (May 2011). "Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation". Pain. 152 (5): 1165–72. doi:10.1016/j.pain.2011.01.049. PMID 21402443. S2CID 21881155.
- ^ Wei H, Karimaa M, Korjamo T, Koivisto A, Pertovaara A (July 2012). "Transient receptor potential ankyrin 1 ion channel contributes to guarding pain and mechanical hypersensitivity in a rat model of postoperative pain". Anesthesiology. 117 (1): 137–48. doi:10.1097/ALN.0b013e31825adb0e. PMID 22588108. S2CID 287826.
- ^ Banzawa N, Saito S, Imagawa T, Kashio M, Takahashi K, Tominaga M, Ohta T (November 2014). "Molecular basis determining inhibition/activation of nociceptive receptor TRPA1 protein: a single amino acid dictates species-specific actions of the most potent mammalian TRPA1 antagonist". The Journal of Biological Chemistry. 289 (46): 31927–39. doi:10.1074/jbc.M114.586891. PMC 4231671. PMID 25271161.
- ^ Koivisto A, Chapman H, Jalava N, Korjamo T, Saarnilehto M, Lindstedt K, Pertovaara A (January 2014). "TRPA1: a transducer and amplifier of pain and inflammation". Basic & Clinical Pharmacology & Toxicology. 114 (1): 50–5. doi:10.1111/bcpt.12138. PMID 24102997.
- ^ Achanta S, Chintagari NR, Brackmann M, Balakrishna S, Jordt SE (September 2018). "TRPA1 and CGRP antagonists counteract vesicant-induced skin injury and inflammation". Toxicology Letters. 293: 140–148. doi:10.1016/j.toxlet.2018.03.007. PMC 5975083. PMID 29535050.
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| TRPA | | Activators |
- 4-Hydroxynonenal
- 4-Oxo-2-nonenal
- 5,6-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 | | Activators |
- ADP-ribose
- BCTC
- Calcium (intracellular)
- CIM-0216
- Cold
- Coolact P
- Cooling Agent 10
- Eucalyptol (eucalyptus)
- Frescolat MGA
- Frescolat ML
- Geraniol
- Hydroxycitronellal
- Icilin
- Linalool
- Menthol (mint)
- PMD 38
- Pregnenolone sulfate
- Rutamarin (Ruta graveolens)
- Steviol glycosides (e.g., stevioside) (Stevia rebaudiana)
- Sweet tastants (e.g., glucose, fructose, sucrose; indirectly)
- Thio-BCTC
- WS-12
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| Blockers | |
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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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See also: Receptor/signaling modulators • Ion channel modulators |