Channelpedia

PubMed 27171974


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPM , TRPM8



Title: Natural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulators.

Authors: Christina M LeGay, Evgueni Gorobets, Mircea Iftinca, Rithwik Ramachandran, Christophe Altier, Darren J Derksen

Journal, date & volume: Org. Lett., 2016 Jun 3 , 18, 2746-9

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/27171974


Abstract
A library of novel structural hybrids of menthol and cubebol was tested for each derivative's ability to interact with the transient receptor potential subfamily melastatin member 8 (TRPM8) channel. This structure-activity relationship study revealed three potent modulators of the TRPM8 ion channel: a novel agonist (4) with an EC50 value of 11 ± 1 μM, an antagonist (15) with an IC50 value of 2 ± 1 μM, and an allosteric modulator (21) that minimized channel desensitization toward menthol. Each of these novel exocyclic olefin analogues of menthol is readily accessible by synthesis and was tested using Ca(2+) assays and electrophysiology.