Physiology and Pharmacology Publications

Title

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

Document Type

Article

Publication Date

6-3-2016

Journal

Organic Letters

Volume

18

Issue

11

First Page

2746

Last Page

2749

URL with Digital Object Identifier

10.1021/acs.orglett.6b01222

Abstract

© 2016 American Chemical Society. 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.

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