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

Fluorescent melatoninergic ligands have been designed by associating the 4-azamelatonin ligands with different fluorophores. The ligands show good affinities for MT 1 and/or MT 2 receptors and substitution of the fluorophore at positions 2 or 5 of the azamelatonin core had a direct impact on the MT...

Full description

Saved in:
Bibliographic Details
Published in:RSC advances 2016, Vol.6 (67), p.62508-62521
Main Authors: Viault, G., Poupart, S., Mourlevat, S., Lagaraine, C., Devavry, S., Lefoulon, F., Bozon, V., Dufourny, L., Delagrange, P., Guillaumet, G., Suzenet, F.
Format: Article
Language:English
Subjects:
Endocrinology and metabolism
Human health and pathology
Life Sciences
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Fluorescent melatoninergic ligands have been designed by associating the 4-azamelatonin ligands with different fluorophores. The ligands show good affinities for MT 1 and/or MT 2 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 MT 1 /MT 2 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.
ISSN:2046-2069
2046-2069
DOI:10.1039/C6RA10812A