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Papers of the Week


Papers: 9 Nov 2019 - 15 Nov 2019


Animal Studies, Pharmacology/Drug Development


2019 Nov 07


Int J Mol Sci


20


22

Characterization of New TRPM8 Modulators in Pain Perception.

Authors

Caro C D, Cristiano C, Avagliano C, Bertamino A, Ostacolo C, Campiglia P, Gomez-Monterrey I, La Rana G, Gualillo O, Calignano A, Russo R
Int J Mol Sci. 2019 Nov 07; 20(22).
PMID: 31703254.

Abstract

Transient Receptor Potential Melastatin-8 (TRPM8) is a non-selective cation channel activated by cold temperature and by cooling agents. Several studies have proved that this channel is involved in pain perception. Although some studies indicate that TRPM8 inhibition is necessary to reduce acute and chronic pain, it is also reported that TRPM8 activation produces analgesia. These conflicting results could be explained by extracellular Ca-dependent desensitization that is induced by an excessive activation. Likely, this effect is due to phosphatidylinositol 4,5-bisphosphate (PIP2) depletion that leads to modification of TRPM8 channel activity, shifting voltage dependence towards more positive potentials. This phenomenon needs further evaluation and confirmation that would allow us to understand better the role of this channel and to develop new therapeutic strategies for controlling pain.