TRPA1 channels as targets for resveratrol and related stilbenoids

[Display omitted] A series of twenty resveratrol analogues was synthesized and tested on TRPA1 and TRPV1 channels. None was able to significantly modulate TRPV1 channels. Conversely, most of them exhibited remarkably higher TRPA1 modulating activity than resveratrol. Optimal potency was observed wit...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-02, Vol.26 (3), p.899-902
Hauptverfasser:	Nalli, Marianna, Ortar, Giorgio, Moriello, Aniello Schiano, Morera, Enrico, Di Marzo, Vincenzo, De Petrocellis, Luciano
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Calcium - metabolism HEK293 Cells Humans Inhibitory Concentration 50 Ion Transport - drug effects Protein Binding Rats Resveratrol Stilbenes - chemistry Stilbenes - metabolism Stilbenes - pharmacology Stilbenoids TRP channels TRPA1 TRPA1 Cation Channel TRPC Cation Channels - chemistry TRPC Cation Channels - genetics TRPC Cation Channels - metabolism TRPV1
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Zusammenfassung:	[Display omitted] A series of twenty resveratrol analogues was synthesized and tested on TRPA1 and TRPV1 channels. None was able to significantly modulate TRPV1 channels. Conversely, most of them exhibited remarkably higher TRPA1 modulating activity than resveratrol. Optimal potency was observed with ortho monoxygenated stilbenes 6 and 17.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2015.12.065