Syracuse

Design, synthesis and biological evaluation of fluorescent ligands for MT 1 and/or MT 2 melatonin receptors

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Viault, G. | Poupart, S. | Mourlevat, S. | Lagaraine, C. | Devavry, S. | Lefoulon, F. | Bozon, Véronique | Dufourny, Laurence | Delagrange, P. | Guillaumet, G. | Suzenet, Franck

Edité par CCSD ; Royal Society of Chemistry -

International audience. Fluorescent melatoninergic ligands have been designed by associating the 4-azamelatonin ligands with different fluorophores. The ligands show good affinities for MT1 and/or MT2 receptors and substitution of the fluorophore at positions 2 or 5 of the azamelatonin core had a direct impact on the MT receptors selectivity while grafting the fluorophores on position N1 produced fluorescent ligands with good affinities for both MT1/MT2 receptors. The optimal position N-1, C-2 or C-5 on the 4-azamelatonin ligand appeared strongly dependent upon the nature of the fluorophore itself.

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