Delta and kappa opioid receptors as suitable drug targets for pain

Research output: Contribution to journalArticle

104 Citations (Scopus)

Abstract

Similar to μ opioid receptors, κ and δ opioid receptors reside in the periphery, the dorsal root ganglion, the spinal cord, and in supraspinal regions associated with pain modulation. Both δ and κ opioid agonists have been shown to activate pain inhibitory pathways in the central nervous system. Yet, currently there are only a few pharmacologic agents that target κ receptors, and none that target δ receptors. Spurred by the need for an efficacious analgesic without the unwanted side effects associated with the typical clinical profile of μ opioid agonists, new research has provided insight into why the development of effective κ and δ opioid receptor agonists has remained elusive thus far, and importantly, how these obstacles may be overcome. For example, for δ opioid agonists to be effective, a state of inflammation may be required as this induces δ opioid receptors to migrate to the surface of neuronal cells and thereby become accessible to δ opioid agonists. Studies have shown that δ opioid agonists can provide relief of inflammatory pain and malignant bone pain. Meanwhile, peripherally restricted κ opioid agonists have been developed to target κ opioid receptors located on visceral and somatic afferent nerves for relief of inflammatory, visceral, and neuropathic chronic pain. The recently shown efficacy of these analgesics combined with a possible lower abuse potential and side effect burden than μ opioid receptor agonists makes δ and peripherally restricted κ opioid receptor agonists promising targets for treating pain.

Original languageEnglish (US)
JournalClinical Journal of Pain
Volume26
Issue numberSUPPL.10
DOIs
StatePublished - Jan 2010

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kappa Opioid Receptor
delta Opioid Receptor
Opioid Receptors
Opioid Analgesics
Pain
Pharmaceutical Preparations
Analgesics
Visceral Afferents
Spinal Ganglia
Neuralgia
Chronic Pain
Spinal Cord
Central Nervous System
Inflammation
Bone and Bones
Research

Keywords

  • δ opioid receptors
  • κ opioid receptors
  • Analgesics
  • Pain
  • Receptor trafficking

ASJC Scopus subject areas

  • Anesthesiology and Pain Medicine
  • Clinical Neurology

Cite this

Delta and kappa opioid receptors as suitable drug targets for pain. / Vanderah, Todd W.

In: Clinical Journal of Pain, Vol. 26, No. SUPPL.10, 01.2010.

Research output: Contribution to journalArticle

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