Current Topics in Medicinal Chemistry

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA


Opioid Receptors and their Ligands

Author(s): Anna Janecka, Jakub Fichna, Tomasz Janecki.


This review gives a historical perspective, summarizing approximately 25 years of research on opioids. The “typical” opioid peptides produced in the brain, “atypical” opioids encrypted in milk protein or hemoglobin sequences, and extremely potent and selective opioids of amphibian origin are described. The main focus is on the structure-activity relationship studies of peptide ligands for three main opioid receptor types (μ, δ, κ), their selectivities and pharmacological activities in vitro. Chemical modifications that led to obtaining potent and selective agonists and antagonists for these receptors are discussed.

Keywords: Opioid peptides, opioid agonists and antagonists, structure-activity relationships, opioid receptor selectivity, receptor binding assay

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

Year: 2004
Page: [1 - 17]
Pages: 17
DOI: 10.2174/1568026043451618