Design, synthesis and biological evaluation of fluorescent ligands for MT1 and/or MT2 melatonin receptors. Issue 67 (29th June 2016)

• Record Type: Journal Article
• Authors: Viault, G.; Poupart, S.; Mourlevat, S.; Lagaraine, C.; Devavry, S.; Lefoulon, F.; Bozon, V.; Dufourny, L.; Delagrange, P.; Guillaumet, G.; Suzenet, F.
• Is Part Of: RSC advances. Volume 6:Issue 67(2016)
• Page Start: 62508
• Page End: 62521
• Publication Date: 2016-06-29
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c6ra10812a
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Fluorescent melatoninergic ligands have been designed by associating the 4-azamelatonin ligands with different fluorophores. 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.