Dynorphin A analogs for the treatment of chronic neuropathic pain

Future Med Chem. 2016;8(2):165-77. doi: 10.4155/fmc.15.164. Epub 2016 Jan 29.

Abstract

Chronic pain is one of the most ubiquitous diseases in the world, but treatment is difficult with conventional methods, due to undesirable side effects of treatments and unknown mechanisms of pathological pain states. The endogenous peptide, dynorphin A has long been established as a target for the treatment of pain. Interestingly, this unique peptide has both inhibitory (opioid in nature) and excitatory activities (nonopioid) in the CNS. Both of these effects have been found to play a role in pain and much work has been done to develop therapeutics to enhance the inhibitory effects. Here we will review the dynorphin A compounds that have been designed for the modulation of pain and will discuss where the field stands today.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Analgesics, Non-Narcotic / therapeutic use
  • Chronic Disease
  • Dynorphins / chemistry
  • Dynorphins / therapeutic use*
  • Humans
  • Neuralgia / drug therapy*
  • Neuralgia / pathology
  • Neurotransmitter Agents / chemistry
  • Neurotransmitter Agents / therapeutic use
  • Receptors, Bradykinin / chemistry
  • Receptors, Bradykinin / metabolism
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
  • Receptors, N-Methyl-D-Aspartate / metabolism
  • Receptors, Opioid, kappa / antagonists & inhibitors
  • Receptors, Opioid, kappa / metabolism
  • Structure-Activity Relationship

Substances

  • Analgesics, Non-Narcotic
  • Neurotransmitter Agents
  • Receptors, Bradykinin
  • Receptors, N-Methyl-D-Aspartate
  • Receptors, Opioid, kappa
  • Dynorphins