In mammals, including humans, the neurohormone melatonin is mainly secreted from the pineal gland at night and acts on two high-affinity G protein-coupled receptors, the melatonin MT(1) and MT(2) receptors. Major functions of melatonin receptors in the brain are the regulation of circadian rhythms and sleep. Correspondingly, the main indications of the currently available drugs for these receptors indicate this as targets. Yet these drugs may not only improve circadian rhythm- and sleep-related…