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MT1 and MT2 Melatonin Receptors: Ligands, Models, Oligomers, and Therapeutic Potential

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Department of Pharmaceutical Chemistry, The German University in Cairo, New Cairo City, 11835 Cairo, Egypt
Inserm, U1016, Institut Cochin, Paris, France
§ CNRS UMR 8104, Paris, France
Univ. Paris Descartes, Sorbonne Paris Cite, Paris, France
Department of Physiology, Institute of Bioscience, University of Sao Paulo, Sao Paulo 05508-090, Brazil
# Dipartimento di Farmacia, Università degli Studi di Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy
Division of Pharmaceutical Sciences, School of Pharmacy, Duquesne University, 421 Mellon Hall, Pittsburgh, Pennsylvania 15282, United States
*Phone: +20 2 2758 1041. Fax: +20 2 2758 1041. E-mail: [email protected]
Cite this: J. Med. Chem. 2014, 57, 8, 3161–3185
Publication Date (Web):November 14, 2013
Copyright © 2013 American Chemical Society

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    Numerous physiological functions of the pineal gland hormone melatonin are mediated via activation of two G-protein-coupled receptors, MT1 and MT2. The melatonergic drugs on the market, ramelteon and agomelatine, as well as the most advanced drug candidates under clinical evaluation, tasimelteon and TIK-301, are high-affinity nonselective MT1/MT2 agonists. A great number of MT2-selective ligands and, more recently, several MT1-selective agents have been reported to date. Herein, we review recent advances in the field focusing on high-affinity agonists and antagonists and those displaying selectivity toward MT1 and MT2 receptors. Moreover, the existing models of MT1 and MT2 receptors as well as the current status in the emerging field of melatonin receptor oligomerization are critically discussed. In addition to the already existing indications, such as insomnia, circadian sleep disorders, and depression, new potential therapeutic applications of melatonergic ligands including cardiovascular regulation, appetite control, tumor growth inhibition, and neurodegenerative diseases are presented.

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    [125I]MLT binding sites in different tissues and cells (Table 1) and receptor dimers and their therapeutic potential (Table 2). This material is available free of charge via the Internet at

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