The best described function of the pineal hormone melatonin is to regulate seasonal reproduction, with its daily production and secretion varying throughout the seasons or the photoperiod. Additionally, a number of behavioral effects of the hormone have been found. This review describes the effects of melatonin in rodent behavior. We focus on: (a) inhibitory effects (sedation, hypnotic activity, pain perception threshold elevation, anti-convulsive activity, anti-anxiety effects); and (b) direct effects on circadian rhythmicity (entrainment, resynchronization, alleviation of jet-lag symptoms, phase-shifting). Most of these effects are clearly time-dependent, with a peak of melatonin activity during the night. One of the possible mechanisms of action for melatonin in the brain is the interaction with the GABAergic system, as suggested by neurochemical and behavioral data. Finally, some pineal hormone effects might be candidates as putative therapies for several human disorders.