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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Tritiated Opioid Receptor Ligands as Radiotracers

Author(s): Geza Toth and Jayapal Reddy Mallareddy

Volume 19, Issue 42, 2013

Page: [7461 - 7472] Pages: 12

DOI: 10.2174/138161281942140105170259

Price: $65


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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