RSC Advances

Design, synthesis and biological ... for MT1 and/or MT2 melatonin receptors

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

Viault G., Poupart S., Mourlevat S., Lagaraine C., Devavry S., Lefoulon F., Bozon V., Dufourny L., Delagrange P., Guillaumet G., Suzenet F

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.

Date de modification : 02 août 2023 | Date de création : 15 juin 2018 | Rédaction : ROBERT V.