You’ve Come a Long Way Baby!

Abstract

Current challenges in opiate pharmacology today are remarkably similar to those almost 40 years ago, when opiate receptors were first identified. There are two key problems to be resolved: (1) We need less-addicting opiates. (2) An understanding of addiction is lacking. Characterization of opiate receptors led to insights into the differentiation of agonists and antagonists. As mixed agonist–antagonists are less addicting, there were hopes for more effective, safer drugs – but these hopes have largely gone unrealized. Appreciation of opioid peptides as endogenous ligands for receptors portended promised further insights into addiction – but we still do not understand the fundamentals of the field. Cloning of receptors and creation of knockouts for them may help answer some of these questions.