Molecular recognition of opioid receptor ligands

Research output: Chapter in Book/Report/Conference proceedingChapter


The cloning of the opioid receptors and subsequent use of recombinant DNA technology have led to many new insights into ligand binding. Instead of focusing on the structural features that lead to increased affinity and selectivity, researchers are now able to focus on why these features are important. Site-directed mutagenesis and chimeric data have often been at the forefront in answering these questions. Herein, we survey pharmacophores of several opioid ligands in an effort to understand the structural requirements for ligand binding and selectivity. Models are presented and compared to illustrate key sites of recognition for both opiate and nonopiate ligands. The results indicate that different ligand classes may recognize different sites within the receptor, suggesting that multiple epitopes may exist for ligand binding and selectivity.

Original languageEnglish (US)
Title of host publicationDrug Addiction
Subtitle of host publicationFrom Basic Research to Therapy
PublisherSpringer New York
Number of pages24
ISBN (Print)9780387766775
StatePublished - Dec 1 2008


  • Opioid
  • chimeric
  • mutagenesis
  • pharmacophore
  • structure-function

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