Molecular mechanisms and regulation of opioid receptor signaling

Annu Rev Pharmacol Toxicol. 2000;40:389-430. doi: 10.1146/annurev.pharmtox.40.1.389.


Cloning of multiple opioid receptors has presented opportunities to investigate the mechanisms of multiple opioid receptor signaling and the regulation of these signals. The subsequent identification of receptor gene structures has also provided opportunities to study the regulation of receptor gene expression and to manipulate the concentration of the gene products in vivo. Thus, in the current review, we examine recent advances in the delineation basis for the multiple opioid receptor signaling, and their regulation at multiple levels. We discuss the use of receptor knockout animals to investigate the function and the pharmacology of these multiple opioid receptors. The reasons and basis for the multiple opioid receptor are addressed.

Publication types

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

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Calcium / metabolism
  • Calcium Channels / physiology
  • Gene Expression Regulation
  • Humans
  • MAP Kinase Signaling System
  • Phosphorylation
  • Potassium Channels / physiology
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / genetics
  • Receptors, Opioid / physiology*
  • Type C Phospholipases / metabolism


  • Calcium Channels
  • Potassium Channels
  • Receptors, Opioid
  • Type C Phospholipases
  • Adenylyl Cyclases
  • Calcium