Melatonin, an endogenous ligand for melatonin receptor, plays an important role in modulating various
physiological activities through acting on different subtypes MT1, MT2 or the binding site MT3. The distinct roles of the
receptor subtypes provide great potential for receptor-specific pharmacological agents. Melatonin has no subtypeselectivity,
so it is very important to develop different subtype-selective ligand for receptor subtype research and drug
development. In order to provide guidance for developing high selective ligand, this paper focused on the MT2-selective
ligands, which developed well in the past years. The MT2-selective ligands, mainly focusing on binding data on MT1 and
MT2 receptor, are reviewed in detail according to their structural classes, and the relative pharmacophore, receptor binding
models and the relationship between the structure of ligand and the affinity along with selectivity for receptor subtype
were discussed, which may facilitate the exploration of more potent and effective MT2-selective ligands.
Keywords: Affinity, melatonin, melatonin receptor, MT2 receptor subtype, MT2-selective ligand, selectivity.
Rights & PermissionsPrintExport