Title: Functional characterization of opioid receptor ligands by aequorin luminescence-based calcium assay
Authors: Fichna, J ×
Gach, K
Piestrzeniewicz, M
Burgeon, E
Poels, Jeroen
Vanden Broeck, Jozef
Janecka, A #
Issue Date: Jun-2006
Publisher: Amer soc pharmacology experimental therapeutics
Series Title: Journal of Pharmacology and Experimental Therapeutics vol:317 issue:3 pages:1150-1154
Abstract: A functional assay, based on aequorin-derived luminescence triggered by receptor-mediated changes in intracellular calcium levels, was used to examine relative potency and efficacy of the mu-opioid agonists endomorphin-1, endomorphin-2, morphiceptin, and their position 3-substituted analogs, as well as the delta-agonist deltorphin-II. The results of the aequorin assay, performed on recombinant cell lines, were compared with those obtained in the functional assay on isolated tissue preparations ( guinea pig ileum and mouse vas deferens). A range of nine opioid peptide ligands produced a similar rank order of potency for the mu- and delta-opioid receptor agonists in both functional assays. The highest potency at the mu- receptor was observed for endomorphin-1, endomorphin-2, and [D-1-Nal(3)] morphiceptin, whereas deltorphin-II was the most potent delta-receptor agonist. In the aequorin assay, the mu- and delta-agonist-triggered luminescence was inhibited by the opioid antagonists naloxone and naltrindole, respectively. We can conclude that the use of the aequorin assay for new mu- and delta-receptor-selective opioid analogs gives pharmacologically relevant data and allows high-throughput compound screening, which does not involve radioactivity or animal tissues. This is the first study that validates the application of this assay in the screening of opioid analogs.
ISSN: 0022-3565
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Animal Physiology and Neurobiology Section - miscellaneous
× corresponding author
# (joint) last author

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