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Characterisation of TRPM8 as a pharmacophore receptor

Matthias Bödding1, Ulrich Wissenbach, Veit Flockerzi

  • 1Experimentelle und Klinische Pharmakologie und Toxikologie, Universität des Saarlandes, D-66421 Homburg, Germany. matthias.boedding@uniklinik-saarland.de

Cell Calcium
|May 23, 2007
PubMed

Insights

New compounds activate the TRPM8 ion channel, which is linked to cancer. These TRPM8 agonists offer potential for pain relief and cancer treatment development.

Area of Science:

  • Molecular Biology
  • Neuroscience
  • Pharmacology

Background:

  • Transient Receptor Potential (TRP) channels, including TRPM8, are temperature-sensitive ion channels.
  • TRPM8 is activated by cold and cooling agents, and its gene is often overexpressed in prostate cancer and other malignancies.

Purpose of the Study:

  • To characterize novel cooling compounds as TRPM8 activators.
  • To evaluate the potency, selectivity, and efficacy of these compounds on TRPM8.
  • To explore their potential as research tools and therapeutic leads.

Main Methods:

  • Calcium (Ca2+) imaging experiments.
  • Whole-cell patch-clamp recordings.
  • Experiments conducted on TRPM8-expressing human embryonic kidney (HEK), prostate cancer (LNCaP), and dorsal root ganglia (DRG) cells.

Main Results:

  • The tested compounds (WS-12, CPS-113, CPS-369, WS-30, WS-148) demonstrated dose-dependent and reversible activation of TRPM8.
  • WS-12 was identified as the most potent TRPM8 activator, showing selectivity for TRPM8 over other TRP channels.
  • Compound efficacy was comparable to known TRPM8 agonist icilin.

Conclusions:

  • The novel carboxamides and other compounds are effective TRPM8 agonists.
  • These compounds serve as valuable tools for studying TRPM8 function.
  • They represent promising chemical leads for developing new TRPM8-targeting drugs for pain management and cancer therapy.

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