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- * Most derivatives functioned similarly to resveratrol or AITC, acting as activators and desensitizers of the TRPA1 channel.
- * Notably, compound 4z (HUHS029) displayed stronger inhibitory effects on TRPA1 than resveratrol, and it showed potential pain-relieving effects in live animal tests.
Article Abstract
A series of 31 resveratrol derivatives was designed, synthesized and evaluated for activation and inhibition of the TRPA1 channel. Most acted as activators and desensitizers of TRPA1 channels like resveratrol or allyl isothiocyanate (AITC). Compound 4z (HUHS029) exhibited higher inhibitory activity than resveratrol with an IC value of 16.1μM. The activity of 4z on TRPA1 was confirmed in TRPA1-expressing HEK293 cells, as well as in rat dorsal root ganglia neurons by a whole cell patch clamp recording. Furthermore, pretreatment with 4z exhibited an analgesic effect on AITC-evoked TRPA1-related pain behavior in vivo.
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| http://dx.doi.org/10.1016/j.bmcl.2017.05.025 | DOI Listing |
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