Gpr171 activation modulates nociceptor functions, alleviating pathologic pain

Pyung Sun Cho, Han Kyu Lee, Young In Choi, Seung In Choi, Ji Yeon Lim, Minseok Kim, Hyun Kim, Sung Jun Jung, Sun Wook Hwang

Research output: Contribution to journalArticlepeer-review

Abstract

Modulation of the function of somatosensory neurons is an important analgesic strategy, requiring the proposal of novel molecular targets. Many G-protein-coupled receptors (GPRs) have been deorphanized, but the receptor locations, outcomes due to their activations, and their signal transductions remain to be elucidated, regarding the somatosensory nociceptor function. Here we report that GPR171, expressed in a nociceptor subpopulation, attenuated pain signals via Gi/o-coupled modulation of the activities of nociceptive ion channels when activated by its newly found ligands. Administration of its natural peptide ligand and a synthetic chemical ligand alleviated nociceptor-mediated acute pain aggravations and also relieved pathologic pain at nanomolar and micromolar ranges. This study suggests that functional alteration of the nociceptor neurons by GPR171 signaling results in pain alleviation and indicates that GPR171 is a promising molecular target for peripheral pain modulation.

Original languageEnglish
Article number256
Pages (from-to)1-17
Number of pages17
JournalBiomedicines
Volume9
Issue number3
DOIs
Publication statusPublished - 2021

Keywords

  • Analgesia
  • GPR171
  • Nociceptor
  • Pain
  • TRP channel

ASJC Scopus subject areas

  • Medicine (miscellaneous)
  • Biochemistry, Genetics and Molecular Biology(all)

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