Abstract
The radioligand binding assay is a powerful method to study the interaction of a ligand with its target. This technique allows not only to determine different pharmacological key parameters such as the affinity and the association and dissociation constants but also to estimate the amount of target expressed in recombinant or endogenous cells or tissues. The current detailed protocols describe the different binding assays (saturation, kinetic, and competition) that can be performed on melatonin receptors using their most commonly used and validated radioligands 2-[125I]-iodomelatonin (2-[125I]-MLT) and [3H]-melatonin ([3H]-MLT).
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Acknowledgement
We thank the members of Jockers Lab who helped to optimize the protocol over the years.
This work was supported by grants from the Fondation Recherche Médicale (Equipe FRM 2019, EQU201903008055); the French National Research Agency (ANR) ANR-19-CE16-0025-01 (Mito-GPCR), ANR-21-CE18-0023-01 (alloGLP1R), Recherches Partenariales et Innovation Biomédicale 2012 “MED-HET-REC-2”; INSERM; CNRS; and La Ligue Contre le Cancer N/Ref: RS19/75-127.
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Gbahou, F., Jockers, R. (2022). 2-[125I]iodomelatonin and [3H]melatonin Binding Assays for Melatonin Receptors. In: Jockers, R., Cecon, E. (eds) Melatonin. Methods in Molecular Biology, vol 2550. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-2593-4_18
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DOI: https://doi.org/10.1007/978-1-0716-2593-4_18
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Online ISBN: 978-1-0716-2593-4
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