Flufenamic acid as an ion channel modulator.
Flufenamic acid as an ion channel modulator.
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DOI：
10.1016/j.pharmthera.2013.01.012
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发表时间：
2013-05
影响因子：
13.5
通讯作者：
Del Negro, Christopher
中科院分区：
文献类型：
--
作者：
Guinamard, Romain;Simard, Christophe;Del Negro, Christopher
自20世纪60年代以来，人们就知道氟芬那酸具有抗炎特性，这是由于它能减少前列腺素的合成。三十年后，氟芬那酸被发现是一种离子通道调节剂。因此，虽然它在医学上的应用减少了，但它在离子通道研究中的应用却扩大了。氟芬那酸通常影响非选择性阳离子通道和氯离子通道，但也调节钾、钙和钠通道，其有效浓度范围从TRPM4通道抑制的10- 6m到双孔外向整流钾通道激活的10- 3m。由于氟芬那酸的作用发展和逆转迅速，是一种方便和广泛使用的工具。然而，考虑到它的目标范围很广，实验结果必须谨慎解释。在这里，我们提供了氟芬那酸靶向离子通道的概述，以帮助解释其在分子、细胞和系统水平上的作用。如果使用得当，氟芬那酸仍然是离子通道研究的有用工具。了解FFA的靶点可能有助于重新评估其生理影响，并使人们对其治疗潜力重新产生兴趣。
Flufenamic acid has been known since the 1960s to have anti-inflammatory properties attributable to the reduction of prostaglandin synthesis. Thirty years later, flufenamic acid appeared to be an ion channel modulator. Thus, while its use in medicine diminished, its use in ionic channel research expanded. Flufenamic acid commonly affects non-selective cation channels and chloride channels, but also modulates potassium, calcium and sodium channels with effective concentrations ranging from 10-6 M in TRPM4 channel inhibition to 10-3 M in two-pore outwardly rectifying potassium channel activation. Because flufenamic acid effects develop and reverse rapidly, it is a convenient and widely used tool. However, given the broad spectrum of its targets, experimental results have to be interpreted cautiously. Here we provide an overview of ion channels targeted by flufenamic acid to aid in interpreting its effects at the molecular, cellular, and systems levels. If it is used with good practices, flufenamic acid remains a useful tool for ion channel research. Understanding the targets of FFA may help reevaluate its physiological impacts and revive interest in its therapeutic potential.
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影响因子：
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作者：
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通讯作者：
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影响因子：
64.8
作者：
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DOI：
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发表时间：
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影响因子：
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作者：
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DOI：
10.1085/jgp.200910316
发表时间：
2010-03
期刊：
The Journal of general physiology
影响因子：
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作者：
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通讯作者：
Sanguinetti MC