2. Academic Validation
  3. Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety

Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety

  • Bioorg Med Chem Lett. 2007 Jan 1;17(1):132-5. doi: 10.1016/j.bmcl.2006.09.077.
Giovanni Appendino 1,  Abdellah Ech-Chahad,  Alberto Minassi,  Sara Bacchiega,  Luciano De Petrocellis,  Vincenzo Di Marzo
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Università del Piemonte Orientale, Viale Ferrucci 33, 28100 Novara, Italy. appendino@pharm.unipmn.it
PMID: 17046253 DOI: 10.1016/j.bmcl.2006.09.077
Abstract

Starting from ROPA (2), analogues of RTX (1a) modified on the acyl side chain were prepared and evaluated for vanilloid activity in HEK-293 cells over-expressing the human recombinant TRPV1. The ROPA motif provided an enhancement of potency sufficient to expand the range of vanillyl surrogates to structural elements (e.g., an unsubstituted phenyl ring) that afford inactive analogues in compounds from the capsaicin series.

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