Basic Information
ID: ALA3421598
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationships of the prototypical TRPM8 agonist icilin.
Authors: De Petrocellis L, Ortar G, Schiano Moriello A, Serum EM, Rusterholz DB.
Abstract: A series of structural analogues of the TRPM8 agonist icilin was prepared. The compounds were examined for their ability to exert agonist or antagonist effects in HEK-293 cells expressing the TRPM8 receptor. Most structural modifications of the icilin structure largely met with diminished TRPM8 agonist activity. Cinnamamide 'open-chain' analogs of icilin, however, demonstrated significant antagonistic actions at the TRPM8 receptor. Optimal potency (IC50=73 nM) was observed in the 3-iodo derivative 18l.
CiteXplore: 25935641
DOI: 10.1016/j.bmcl.2015.04.032
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets