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Luciano De Petrocellis-CNS&ND-MS

semanticscholar(2016)

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摘要
DOI: http://dx.doi.org/10.1016/j.ienj.2015. 05.007 Abstract: Eleven compounds belonging to the chalcone family were tested for their ability to activate and subsequently desensitize the rat transient receptor potential ankyrin 1 cation channel, subfamily A, member 1 (TRPA1) in a heterologous expression system. Four of the tested compounds were more potent than the TRPA1 agonist mustard oil, and showed also a strong desensitizing effect. Some chalcone compounds were not pungent in the eye-wiping assay and quite remarkably inhibited in a long-lasting and dose-dependent manner the mustard oil-induced response in the formalin test. Chalcones can be considered as novel candidates for the development of anti-hyperalgesic preparations based on TRPA1 desensitization.
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