Melatonin, the pineal gland
hormone, is widely distributed in mammalian tissues and exerts its action via two
melatonin receptor sub-types, MT(1) and MT(2).
Melatonin is known to play functional roles in regulating circadian rhythms and seasonal reproduction. In recent years, growing evidence has also linked
melatonin to a variety of other body systems and disease states, thus highlighting its significance as a therapeutic agent. However, due to its properties,
melatonin is ineffective in clinical use, thus prompting the development of melatoninergic
ligands that mimic the actions of
melatonin but in a manner that is more potent and specific for
melatonin receptors. An additional focus has been to develop
ligands that exhibit receptor subtype selectivity. While there are over seventy patents on melatoninergic
ligands, success in developing therapeutically effective melatoninergic
ligands have been varied. However, the recent approval of
Ramelteon for treatment of
sleep disorders and the evaluation of other compounds in clinical trials have highlighted their clinical importance. In this review an overview of recently developed novel melatoninergic
ligands is provided including recently filed patents and compounds undergoing clinical evaluation.