TRPM8 as a target for analgesia

Research output: Chapter in Book/Report/Conference proceedingChapter (peer-reviewed)peer-review

Abstract / Description of output

TRPM8 is a cation channel expressed in a small subpopulation of sensory neurons, which
detect innocuous cooling and mostly lack characteristics of nociceptors. Whether TRPM8
normally contributes to noxious cold sensing is debatable as few TRPM8-positive neurons
co-express nociceptive markers. TRPM8 is a promising analgesic target. TRPM8 agonists
cause analgesia in chronic pain states, by TRPM8-expressing afferents gating-out a wide
range of hypersensitive pain responses in spinal cord. TRPM8 antagonists may attenuate
exaggerated responses to mild cooling during chronic pain but will not achieve generalised
analgesia as they can only block cool detection, not the clinically problematic
hypersensitivity to other sensory modalities. Biochemical and physiological properties of
TRPM8, the chemistry of TRPM8 ligands, intracellular modulation of TRPM8 and the
neurobiological consequences of TRPM8 activation are discussed, with a view to future
improvements in therapeutic targeting.
Original languageEnglish
Title of host publicationTRP channels as therapeutic targets - from basic science to clinical use
EditorsArpad Szallasi
Place of PublicationWaltham, MA, USA
PublisherAcademic Press
Number of pages24
ISBN (Print)978-0-12-420024-1
Publication statusPublished - 17 Nov 2015

Keywords / Materials (for Non-textual outputs)

  • TRPM8, pain, analgesia, cool sensing, 5-HT1B receptor, intracellular signalling


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