Abstract
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
Current Topics in Medicinal Chemistry
Title: Opioid Receptors and their Ligands
Volume: 4 Issue: 1
Author(s): Anna Janecka, Jakub Fichna and Tomasz Janecki
Affiliation:
Keywords: Opioid peptides, opioid agonists and antagonists, structure-activity relationships, opioid receptor selectivity, receptor binding assay
Abstract: 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.
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Cite this article as:
Janecka Anna, Fichna Jakub and Janecki Tomasz, Opioid Receptors and their Ligands, Current Topics in Medicinal Chemistry 2004; 4 (1) . https://dx.doi.org/10.2174/1568026043451618
DOI https://dx.doi.org/10.2174/1568026043451618 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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