Melatonin, the primary hormone of the pineal gland, is a powerful "chronobiotic" that helps maintain the body's normal circadian rhythms. In individuals who have difficulty sleeping or who have altered circadian rhythms because of jet lag or night shift work, melatonin supplementation promotes the resynchronization of this cycle. Supplementation can also benefit those whose difficulty sleeping is caused by the aging-related decrease in the body's ability to synthesize melatonin from the amino acid tryptophan. Research indicates melatonin exerts its sleep-promoting efficacy by decreasing the amount of time needed to fall asleep, by promoting the ability to stay asleep, and by enhancing the depth of sleep.

Melatonin administration from 0.3 mg to 5.0 mg has been shown to exert a sedative-like effect. When supplemented prior to the onset of the body's normal melatonin secretion, even a low amount of melatonin can promote sleep. Melatonin apparently enhances the effect of gamma-aminobutyric acid (GABA) via direct interaction with GABA receptors, thus resulting in relaxation. Melatonin also has significant antioxidant activity. Adequate melatonin levels have been reported to be a positive factor in cardiovascular, neuroendocrine, GI, and bone health.

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