119614-71-0Relevant articles and documents
Natural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulators
Legay, Christina M.,Gorobets, Evgueni,Iftinca, Mircea,Ramachandran, Rithwik,Altier, Christophe,Derksen, Darren J.
, p. 2746 - 2749 (2016)
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 Ca2+ assays and electrophysiology.