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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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Supplementary files

Article information


Submitted
29 Apr 2016
Accepted
21 Jun 2016
First published
23 Jun 2016

RSC Adv., 2016,6, 62508-62521
Article type
Paper

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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