title: 3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators.
abstract: Following the recent identification of the naturally occurring 3-ylidene-4,5-dihydrophthalide ligustilide and its oxidation product dehydroligustilide as novel TRPA1 modulators, a series of seventeen 3-ylidenephthalides was synthesized and tested on TRPA1 and TRPM8 channels. Most of these compounds acted as strong modulators of the two channel types with EC50 and/or IC50 values distinctly lower than those of the reference compounds.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: giorgio.ortar@uniroma1.it.
authors.forename: Giorgio
authors.initials: G
authors.lastname: Ortar
authors.forename: Aniello
authors.initials: A
authors.lastname: Schiano Moriello
authors.forename: Enrico
authors.initials: E
authors.lastname: Morera
authors.forename: Marianna
authors.initials: M
authors.lastname: Nalli
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Di Marzo
authors.forename: Luciano
authors.initials: L
authors.lastname: De Petrocellis
mesh_terms: D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000737:chemistry; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D010084:Oxidation-Reduction; D011485:Protein Binding; D051381:Rats; D000074025:TRPA1 Cation Channel; D050052:TRPC Cation Channels / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D050053:TRPM Cation Channels / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D001572:Benzofurans; D000074025:TRPA1 Cation Channel; D050052:TRPC Cation Channels; D050053:TRPM Cation Channels; C480976:Trpa1 protein, rat; C498947:Trpm8 protein, rat; C027820:ligustilide; C082022:phthalide; D015107:4-Butyrolactone
keywords: 3-Ylidenephthalides; TRPA1; TRPM8; Transient receptor potential channels