Melatonin receptor ligands: A pharmaco-chemical perspective.

Journal of Pineal Research
Jean A BoutinDarius P Zlotos

Abstract

Melatonin MT1 and MT2 receptor ligands have been vigorously explored for the last 4 decades. Inspection of approximately 80 publications in the field revealed that most melatonergic ligands were structural analogues of melatonin combining three essential features of the parent compound: an aromatic ring bearing a methoxy group and an amide side chain in a relative arrangement similar to that present in melatonin. While several series of MT2 -selective agents-agonists, antagonists, or partial agonists-were reported, the field was lacking MT1 -selective agents. Herein, we describe various approaches toward the development of melatonergic ligands, keeping in mind that most of the molecules/pharmacophores obtained were essentially melatonin copies, even though diverse tri- or tetra-cyclic compounds were explored. In addition to lack of structural diversity, only few studies examined the activity of the reported melatonergic ligands in vivo. Moreover, an extensive pharmacological characterization including biopharmaceutical stability, pharmacokinetic properties, specificity toward other major receptors to name a few remained scarce. For example, many of the antagonists described were not stable in vivo, were not selective for the me...Continue Reading

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Citations

Sep 10, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Gian Marco ElisiGilberto Spadoni
Oct 28, 2020·Journal of Pineal Research·Jean A Boutin, Ralf Jockers
Aug 27, 2021·Journal of Pineal Research·Ko-Hsiu LuShun-Fa Yang
Dec 22, 2021·Journal of Chemical Information and Modeling·Gian Marco ElisiSilvia Rivara
Oct 29, 2021·The Journal of Pharmacology and Experimental Therapeutics·Preety Shabajee-AlibayCeline Legros
Jan 22, 2022·Médecine sciences : M/S·Jean A Boutin

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