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. 2007 Jan 1;17(1):132-5.
doi: 10.1016/j.bmcl.2006.09.077. Epub 2006 Sep 29.

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

Giovanni Appendino  1 , Abdellah Ech-Chahad, Alberto Minassi, Sara Bacchiega, Luciano De Petrocellis, Vincenzo Di Marzo
Affiliations

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

Giovanni Appendino et al. Bioorg Med Chem Lett. .

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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