Endogenous lipid-derived ligands for sensory TRP ion channels and their pain modulation

Sangsu Bang, Sungjae Yoo, Uhtaek Oh, Sun Wook Hwang

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

Environmental or internal noxious stimuli excite the primary sensory nerves in our body. The sensory nerves relay these signals by electrical discharges to the brain, leading to pain perception. Six transient receptor potential (TRP) ion channels are expressed in the sensory nerve terminals and play a crucial role in sensing diverse noxious stimuli. Cation influx through activated TRP ion channels depolarizes the plasma membrane, resulting in neuronal excitation and pain. Natural and synthetic compounds have been found to act on these sensory TRP channels to alter the nociception. Evidence is growing that lipidergic substances are also cable of modifying TRP ion channel activity by direct binding. Here, we focus on endogenously generated lipids that modulate the sensory TRP activities. Unsaturated fatty acids or their metabolites via lipoxygenase, cyclooxygenase or epoxygenase are able to modulate (activate, inhibit or potentiate) the function of specific TRPs. Isoprene lipids, diacylglycerol, resolvin, and lysophospholipids also show distinct activities on sensory TRP channels. Outcomes caused by the interactions between sensory TRPs and lipid ligands are also discussed. The knowledge we collected here implicates that information on lipidergic ligands may contribute to our understanding of peripheral pain mechanism and provide an opportunity to design novel therapeutic strategies.

Original languageEnglish
Pages (from-to)1509-1520
Number of pages12
JournalArchives of Pharmacal Research
Volume33
Issue number10
DOIs
Publication statusPublished - 2010 Oct 1

Fingerprint

Transient Receptor Potential Channels
Sensory Receptor Cells
Ion Channels
Modulation
Ligands
Lipids
Pain
Lysophospholipids
Lipoxygenase
Diglycerides
Cell membranes
Prostaglandin-Endoperoxide Synthases
Metabolites
Unsaturated Fatty Acids
Pain Perception
Nociception
Cations
Brain
Cables
Cell Membrane

Keywords

  • Endogenous ligand
  • Inflammation
  • Lipidergic substance
  • Pain
  • Sensory neurons
  • Transient receptor potential ion channel

ASJC Scopus subject areas

  • Drug Discovery
  • Molecular Medicine
  • Organic Chemistry

Cite this

Endogenous lipid-derived ligands for sensory TRP ion channels and their pain modulation. / Bang, Sangsu; Yoo, Sungjae; Oh, Uhtaek; Hwang, Sun Wook.

In: Archives of Pharmacal Research, Vol. 33, No. 10, 01.10.2010, p. 1509-1520.

Research output: Contribution to journalArticle

Bang, Sangsu ; Yoo, Sungjae ; Oh, Uhtaek ; Hwang, Sun Wook. / Endogenous lipid-derived ligands for sensory TRP ion channels and their pain modulation. In: Archives of Pharmacal Research. 2010 ; Vol. 33, No. 10. pp. 1509-1520.
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