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.
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