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 pain response in the formalin test.
Chalcones can be considered as novel candidates for the development of antihyperalgesic
preparations based on TRPA1 desensitization.
Keywords: Chalcones, eye wiping, neuropathic pain, pain, TRPA1.
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