2. Academic Validation
  3. TRPA1 channels as targets for resveratrol and related stilbenoids

TRPA1 channels as targets for resveratrol and related stilbenoids

  • Bioorg Med Chem Lett. 2016 Feb 1;26(3):899-902. doi: 10.1016/j.bmcl.2015.12.065.
Marianna Nalli 1,  Giorgio Ortar 2,  Aniello Schiano Moriello 3,  Enrico Morera 2,  Vincenzo Di Marzo 3,  Luciano De Petrocellis 4
Affiliations

Affiliations

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: [email protected].
  • 2 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
  • 3 Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy.
  • 4 Endocannabinoid Research Group, Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, via dei Campi Flegrei 34, 80078 Pozzuoli (Napoli), Italy. Electronic address: [email protected].
PMID: 26750258 DOI: 10.1016/j.bmcl.2015.12.065
Abstract

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.

Keywords

Resveratrol; Stilbenoids; TRP channels; TRPA1; TRPV1.

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