GSK1702934A |
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3-[1-(5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-2-carbonyl)piperidin-4-yl]-1H-benzimidazol-2-one
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| Formula | C22H25N3O2S |
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| Molar mass | 395.52 g·mol−1 |
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C1CCC2=C(CC1)SC(=C2)C(=O)N3CCC(CC3)N4C5=CC=CC=C5NC4=O
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InChI=1S/C22H25N3O2S/c26-21(20-14-15-6-2-1-3-9-19(15)28-20)24-12-10-16(11-13-24)25-18-8-5-4-7-17(18)23-22(25)27/h4-5,7-8,14,16H,1-3,6,9-13H2,(H,23,27) Key:AXWRAIIIBRLXBP-UHFFFAOYSA-N
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GSK1702934A is a chemical compound which acts as an activator of the TRPC family of calcium channels, with selectivity for the TRPC3 and TRPC6 subtypes. It has been used to investigate the role of TRPC channels in heart function and regulation of blood pressure, as well as roles in the brain.[1][2][3][4]
References
- ^ Xu X, Lozinskaya I, Costell M, Lin Z, Ball JA, Bernard R, Behm DJ, Marino JP, Schnackenberg (2013). "CG Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists". Biophysical Journal. 104 (2): 454a. Bibcode:2013BpJ...104..454X. doi:10.1016/j.bpj.2012.11.2513.
- ^ Doleschal B, Primessnig U, Wölkart G, Wolf S, Schernthaner M, Lichtenegger M, Glasnov TN, Kappe CO, Mayer B, Antoons G, Heinzel F, Poteser M, Groschner K (April 2015). "TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1". Cardiovascular Research. 106 (1): 163–73. doi:10.1093/cvr/cvv022. PMC 4362401. PMID 25631581.
- ^ Tiapko O, Groschner K (July 2018). "TRPC3 as a Target of Novel Therapeutic Interventions". Cells. 7 (7): 83. doi:10.3390/cells7070083. PMC 6071100. PMID 30037143.
- ^ Wang Y, Liu L, Tao H, Wen L, Qin S (December 2020). "TRPC6 participates in the development of blood pressure variability increase in sino-aortic denervated rats". Heart and Vessels. 35 (12): 1755–1765. doi:10.1007/s00380-020-01682-1. PMID 32844288. S2CID 221309937.
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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 |