Recent advances in selective opioid receptor agonists and antagonists

Opioid analgesics provide outstanding benefits for relief of severe pain. The mechanisms of the analgesia accompanied with some side effects have been investigated by many scientists to shed light on the complex biological processes at the molecular level. New opioid drugs and therapies with more desirable properties can be developed on the bases of accurate insight of the opioid ligand–receptor interaction and clear knowledge of the pharmacological behavior of opioid receptors and the associated proteins. Toward this goal, recent advances in selective opioid receptor agonists and antagonists including opioid ligand–receptor interactions are summarized in this review article. © 2003 Wiley Periodicals, Inc. Med Res Rev, 24, No. 2, 182–212, 2004