Channelpedia

PubMed 22257892


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPA , TRPA1 , TRPV , TRPV1



Title: Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators.

Authors: Enrico Morera, Luciano De Petrocellis, Ludovica Morera, Aniello Schiano Moriello, Marianna Nalli, Vincenzo Di Marzo, Giorgio Ortar

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Feb 15 , 22, 1674-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22257892


Abstract
In order to explore the structural determinants for the TRPV1 and TRPA1 agonist properties of gingerols, a series of nineteen analogues (1b-5) of racemic [6]-gingerol (1a) was synthesized and tested on TRPV1 and TRPA1 channels. The exploration of the structure-activity relationships, by modulating the three pharmacophoric regions of [6]-gingerol, led to the identification of some selective TRPV1 agonists/desensitizers of TRPV1 channels (3a, 3f, and 4) and of some full TRPA1 antagonists (2c, 2d, 3b, and 3d).