Development of Agonists and Antagonists for Melatonin Receptors

  • Darius P. ZlotosEmail author


Numerous physiological actions of melatonin are mediated by two G-protein-coupled MT1 and MT2 receptors. The melatonergic drugs on the market, ramelteon and agomelatine, as well as the most advanced melatonergic ligands under clinical evaluation, tasimelteon and TIK-301, are high-affinity nonselective MT1 and MT2 agonists. However, exploring the exact physiological role of the MT1 and MT2 melatonin receptors requires subtype-selective MT1 and MT2 ligands. This chapter summarizes the progress in the development of melatonergic agonists and antagonists focusing on high-affinity and subtype-selective agents.


Melatonin Melatonin receptor agonists Melatonin receptor antagonists Melatonin receptor partial agonists MT1 receptors MT2 receptors Selective ligands 


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© Springer India 2014

Authors and Affiliations

  1. 1.Department of Pharmaceutical Chemistry, Faculty of Pharmacy and BiotechnologyThe German University in CairoNew Cairo CityEgypt

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