Modulation of pain transmission by G-protein-coupled receptors

Hui Lin Pan, Zi Zhen Wu, Hong Yi Zhou, Shao Rui Chen, Hong Mei Zhang, De Pei Li

Research output: Contribution to journalReview articlepeer-review


The heterotrimeric G-protein-coupled receptors (GPCR) represent the largest and most diverse family of cell surface receptors and proteins. GPCR are widely distributed in the peripheral and central nervous systems and are one of the most important therapeutic targets in pain medicine. GPCR are present on the plasma membrane of neurons and their terminals along the nociceptive pathways and are closely associated with the modulation of pain transmission. GPCR that can produce analgesia upon activation include opioid, cannabinoid, α2-adrenergic, muscarinic acetylcholine, γ-aminobutyric acidB (GABAB), groups II and III metabotropic glutamate, and somatostatin receptors. Recent studies have led to a better understanding of the role of these GPCR in the regulation of pain transmission. Here, we review the current knowledge about the cellular and molecular mechanisms that underlie the analgesic actions of GPCR agonists, with a focus on their effects on ion channels expressed on nociceptive sensory neurons and on synaptic transmission at the spinal cord level.

Original languageEnglish (US)
Pages (from-to)141-161
Number of pages21
JournalPharmacology and Therapeutics
Issue number1
StatePublished - Jan 2008
Externally publishedYes


  • Analgesia
  • Dorsal root ganglion
  • G-protein-coupled inwardly rectifying K channels
  • Spinal cord
  • Synaptic transmission
  • Voltage-gated Ca channels

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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