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Issue 67, 2016, Issue in Progress
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Design, synthesis and biological evaluation of fluorescent ligands for MT1 and/or MT2 melatonin receptors

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Abstract

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.

Graphical abstract: Design, synthesis and biological evaluation of fluorescent ligands for MT1 and/or MT2 melatonin receptors

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Publication details

The article was received on 29 Apr 2016, accepted on 21 Jun 2016 and first published on 23 Jun 2016


Article type: Paper
DOI: 10.1039/C6RA10812A
Citation: RSC Adv., 2016,6, 62508-62521

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    Design, synthesis and biological evaluation of fluorescent ligands for MT1 and/or MT2 melatonin receptors

    G. Viault, S. Poupart, S. Mourlevat, C. Lagaraine, S. Devavry, F. Lefoulon, V. Bozon, L. Dufourny, P. Delagrange, G. Guillaumet and F. Suzenet, RSC Adv., 2016, 6, 62508
    DOI: 10.1039/C6RA10812A

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