Referenced in: none

Automatically associated channels: TRP , TRPM , TRPM8

Title: Structure-activity relationships of the prototypical TRPM8 agonist icilin.

Authors: Luciano De Petrocellis, Giorgio Ortar, Aniello Schiano Moriello, Eric M Serum, David B Rusterholz

Journal, date & volume: Bioorg. Med. Chem. Lett., 2015 Jun 1 , 25, 2285-90

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25935641

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.