The opioid receptors as targets for drug abuse medication

Br J Pharmacol. 2015 Aug;172(16):3964-79. doi: 10.1111/bph.13190. Epub 2015 Jun 26.


The endogenous opioid system is largely expressed in the brain, and both endogenous opioid peptides and receptors are present in areas associated with reward and motivation. It is well known that this endogenous system plays a key role in many aspects of addictive behaviours. The present review summarizes the modifications of the opioid system induced by chronic treatment with drugs of abuse reported in preclinical and clinical studies, as well as the action of opioid antagonists and agonists on the reinforcing effects of drugs of abuse, with therapeutic perspectives. We have focused on the effects of chronic psychostimulants, alcohol and nicotine exposure. Taken together, the changes in both opioid peptides and opioid receptors in different brain structures following acute or chronic exposure to these drugs of abuse clearly identify the opioid system as a potential target for the development of effective pharmacotherapy for the treatment of addiction and the prevention of relapse.

Publication types

  • Review

MeSH terms

  • Alcohol Drinking / metabolism
  • Animals
  • Central Nervous System Stimulants / pharmacology
  • Cocaine / pharmacology
  • Ganglionic Stimulants / pharmacology
  • Humans
  • Nicotine / pharmacology
  • Receptors, Opioid / metabolism*
  • Substance-Related Disorders / drug therapy
  • Substance-Related Disorders / metabolism*


  • Central Nervous System Stimulants
  • Ganglionic Stimulants
  • Receptors, Opioid
  • Nicotine
  • Cocaine