Activation of the transient receptor potential vanilloid-1 (TRPV1) channel opens the gate for pain relief

Research output: Contribution to journalComment/debate

18 Citations (Scopus)

Abstract

Pharmacological modulation of the transient receptor potential vanilloid-1 (TRPV1) receptor function offers a promising means of producing pain relief at the level of the primary sensory neuron. In this issue of the BJP, the pharmacological approaches and the available experimental data that focus on the TRPV1 receptor to achieve therapeutically useful alleviation of pain and inflammation are reviewed. The potentials to inactivate TRPV1 receptor function by site- and modality-specific TRPV1 antagonists, uncompetitive TRPV1 blockers and drugs interfering with TRPV1 sensitization, are evaluated. A crucial issue of producing pain relief at the level of the nocisensor remains whether it can be achieved solely through inactivation of the TRPV1 receptor or TRPV1 agonist-induced defunctionalization of the whole primary afferent neuron is required. The accumulated evidence indicates that both pharmacological modulation of the intracellular trafficking of the TRPV1 receptor and defunctionalization of the nocisensors by TRPV1 agonists are promising novel approaches to tame the TRPV1 receptor.

Original languageEnglish
Pages (from-to)1139-1141
Number of pages3
JournalBritish journal of pharmacology
Volume155
Issue number8
DOIs
Publication statusPublished - Dec 25 2008

Keywords

  • Analgesia
  • Capsaicin
  • Lipid raft
  • Neurodegeneration
  • Neuropeptides
  • Pain
  • TRPV1
  • Vanilloid

ASJC Scopus subject areas

  • Pharmacology

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