Abstract
Tritiated opioid ligands are essential tools for the identification of opioid receptors. This review deals with the syntheses of tritiated opioid peptide derivatives, including enkephalins, dynorphins, dermorphins, deltorphins and endomorphins, and also discusses tritium-labeled nonpeptide opioids. It additionally focuses on the relevance of tritium-labeled opioid compounds as research tools for investigating opioid receptor pharmacology. Agonists and antagonists are used for the characterization of new opioid ligands by means of radioreceptor binding assays. Further topics covered in this review are the distribution of the endogenous peptides in the central nervous system and peripheral tissues, and degradation studies of opioids in brain membrane preparations and the blood.
Keywords: Radiotracers, tritium, opioid receptors, opiates, opioid peptides.
Current Pharmaceutical Design
Title:Tritiated Opioid Receptor Ligands as Radiotracers
Volume: 19 Issue: 42
Author(s): Geza Toth and Jayapal Reddy Mallareddy
Affiliation:
Keywords: Radiotracers, tritium, opioid receptors, opiates, opioid peptides.
Abstract: Tritiated opioid ligands are essential tools for the identification of opioid receptors. This review deals with the syntheses of tritiated opioid peptide derivatives, including enkephalins, dynorphins, dermorphins, deltorphins and endomorphins, and also discusses tritium-labeled nonpeptide opioids. It additionally focuses on the relevance of tritium-labeled opioid compounds as research tools for investigating opioid receptor pharmacology. Agonists and antagonists are used for the characterization of new opioid ligands by means of radioreceptor binding assays. Further topics covered in this review are the distribution of the endogenous peptides in the central nervous system and peripheral tissues, and degradation studies of opioids in brain membrane preparations and the blood.
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Cite this article as:
Toth Geza and Mallareddy Reddy Jayapal, Tritiated Opioid Receptor Ligands as Radiotracers, Current Pharmaceutical Design 2013; 19 (42) . https://dx.doi.org/10.2174/138161281942140105170259
DOI https://dx.doi.org/10.2174/138161281942140105170259 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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