Analysis of opioid efficacy, tolerance, addiction and dependence from cell culture to human

Br J Pharmacol. 2011 Oct;164(4):1322-34. doi: 10.1111/j.1476-5381.2011.01335.x.


Opioid agonists are the most effective treatment for pain, but their use is limited by side effects, tolerance and fears of addiction and dependence. A major goal of opioid research is to develop agonists that have high analgesic efficacy and a low profile for side effects, tolerance, addiction and dependence. Unfortunately, there is a serious lack of experimental data comparing the degree to which different opioids produce these effects in humans. In contrast, a wide range of experimental techniques from heterologous expression systems to behaviour assessment in whole animals have been developed to study these problems. The objective of this review is to describe and evaluate these techniques as they are used to study opioid efficacy, tolerance, addiction and dependence.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Analgesics, Opioid / adverse effects
  • Analgesics, Opioid / pharmacology
  • Analgesics, Opioid / therapeutic use*
  • Animals
  • Behavior, Addictive*
  • Behavior, Animal / drug effects
  • Cell Culture Techniques
  • Drug Tolerance*
  • Humans
  • Opioid-Related Disorders / epidemiology*
  • Pain / chemically induced
  • Pain / drug therapy*
  • Research Design


  • Analgesics, Opioid