生物活性 | |||
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描述 | Transient receptor potential ankyrin 1 (TRPA1) is a Ca2+-permeable nonselective cation channel expressed in neuronal and nonneuronal cells and plays an important role in acute and inflammatory pain. Diphenyleneiodonium chloride (DPI), a NADPH oxidase (NOX) inhibitor, also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Application of DPI at 0.03-10 μM induced a Ca2+ response in HEK-TRPA1 cells in a concentration-dependent manner. In inflammatory human synoviocytes where TRPA1 is functionally expressed, 3 μM DPI evoked a Ca2+ response when cells were treated with IL1α suggesting that DPI activates endogenous TRPA1 expressed in human synoviocytes[3]. In human RPE cell line ARPE-19 cells, DPI (0.1, 1, and 10 μM) resulted in a significant decrease of cell proliferation, without vacuolation and detachment of the cells from the dish. Significantly increased level of p53 was detected at 4 h after treatment of DPI[4]. In mice, intraplantar injection of 2 mM DPI caused a pain-related response which was inhibited by preadministration with HC (a selective TRPA1 antagonist, HC-030031)[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.90mL 3.18mL 1.59mL |
31.79mL 6.36mL 3.18mL |
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