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

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.
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https://hal.inrae.fr/hal-03170796
Contributor : Eric Marchoux <>
Submitted on : Tuesday, March 16, 2021 - 2:32:02 PM
Last modification on : Wednesday, May 19, 2021 - 10:37:29 AM

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G. Viault, S. Poupart, S. Mourlevat, C. Lagaraine, S. Devavry, et al.. Design, synthesis and biological evaluation of fluorescent ligands for MT 1 and/or MT 2 melatonin receptors. RSC Advances, Royal Society of Chemistry, 2016, 6 (67), pp.62508-62521. ⟨10.1039/C6RA10812A⟩. ⟨hal-03170796⟩

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