Molecular regulation of opioid receptors

Recept Channels. 1997;5(3-4):231-5.


Opioid actions are initiated at membrane receptors which couple to cellular effectors through G protein-mediated pathways. In the central nervous system opioids reduce neuronal activity through the inhibition of voltage-dependent Ca2+ channels, the activation of K+ channels and the inhibition of adenylyl cyclase. A significant clinical limitation to opioid therapy is the development of tolerance, a biological event that has been linked to agonist effects at the receptor level. Molecular studies on the consequences of opioid receptor regulation will provide a better understanding of the cellular mechanisms involved in the agonist-mediated events in tolerance development.

Publication types

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

MeSH terms

  • Animals
  • Humans
  • Receptors, Opioid / metabolism*


  • Receptors, Opioid