Biased Opioid Receptor Ligands: Gain without Pain

Trends Endocrinol Metab. 2017 Apr;28(4):247-249. doi: 10.1016/j.tem.2017.01.001. Epub 2017 Jan 16.

Abstract

Kappa opioid receptor (κ-OR) agonists are promising therapeutic candidates for pain and itch; however, they also exhibit the adverse effects of sedation and dysphoria. A recent study has demonstrated that a G protein-biased agonist for κ-OR provides effective pain and itch relief without causing sedation or dysphoria, in animal models.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics, Opioid / adverse effects
  • Analgesics, Opioid / therapeutic use
  • Animals
  • Humans
  • Models, Animal
  • Pain / drug therapy*
  • Pain / metabolism*
  • Pain / prevention & control
  • Receptors, Opioid / agonists*
  • Receptors, Opioid / metabolism*

Substances

  • Analgesics, Opioid
  • Receptors, Opioid