Title : Discovery of non-electrophilic capsaicinoid-type TRPA1 ligands.

Pub. Date : 2015 Mar 1

PMID : 25666822






6 Functional Relationships(s)
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1 Discovery of non-electrophilic capsaicinoid-type TRPA1 ligands. Capsaicin transient receptor potential cation channel subfamily A member 1 Homo sapiens
2 Replacement of the benzylamide motif of synthetic capsaicin (nonivamide, 1c) with a tetrazole moiety was detrimental for TRPV1 binding, but unexpectedly generated a potent and non-electrophilic TRPA1 agonist (4a). Capsaicin transient receptor potential cation channel subfamily A member 1 Homo sapiens
3 These observations show that the capsaicinoid pharmacophore displays orthogonal structure-activity relationships for TRPV1 and TRPA1 binding, and suggest the possibility of obtaining compounds with dual TRPV1/TRPA1 modulatory properties by exploration of the chemical space around the capsaicin motif. Capsaicin transient receptor potential cation channel subfamily A member 1 Homo sapiens
4 These observations show that the capsaicinoid pharmacophore displays orthogonal structure-activity relationships for TRPV1 and TRPA1 binding, and suggest the possibility of obtaining compounds with dual TRPV1/TRPA1 modulatory properties by exploration of the chemical space around the capsaicin motif. Capsaicin transient receptor potential cation channel subfamily A member 1 Homo sapiens
5 These observations show that the capsaicinoid pharmacophore displays orthogonal structure-activity relationships for TRPV1 and TRPA1 binding, and suggest the possibility of obtaining compounds with dual TRPV1/TRPA1 modulatory properties by exploration of the chemical space around the capsaicin motif. Capsaicin transient receptor potential cation channel subfamily A member 1 Homo sapiens
6 These observations show that the capsaicinoid pharmacophore displays orthogonal structure-activity relationships for TRPV1 and TRPA1 binding, and suggest the possibility of obtaining compounds with dual TRPV1/TRPA1 modulatory properties by exploration of the chemical space around the capsaicin motif. Capsaicin transient receptor potential cation channel subfamily A member 1 Homo sapiens