2. Academic Validation
  3. Structure-activity relationships of the prototypical TRPM8 agonist icilin

Structure-activity relationships of the prototypical TRPM8 agonist icilin

  • Bioorg Med Chem Lett. 2015 Jun 1;25(11):2285-90. doi: 10.1016/j.bmcl.2015.04.032.
Luciano De Petrocellis 1,  Giorgio Ortar 2,  Aniello Schiano Moriello 3,  Eric M Serum 4,  David B Rusterholz 5
Affiliations

Affiliations

  • 1 Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council, Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Naples, Italy. Electronic address: l.depetrocellis@icb.cnr.it.
  • 2 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza-Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
  • 3 Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council, Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Naples, Italy.
  • 4 Department of Chemistry and Biochemistry, North Dakota State University, Fargo, ND 58108, United States.
  • 5 Department of Chemistry, University of Wisconsin-River Falls, 410 S. Third St., River Falls, WI 54022, United States.
PMID: 25935641 DOI: 10.1016/j.bmcl.2015.04.032
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.

Keywords

Icilin; TRPM8; TRPV1; Thermo-TRP channels.

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