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Melatonin, an indoleamine, is a natural compound produced by various organisms, including bacteria and eukaryotes. [1] Its discovery in 1958 by Aaron B. Lerner and colleagues stemmed from the isolation of a substance from the pineal gland of cows that could induce skin lightening in common frogs.
The melatonin receptors are G protein-coupled receptors and are expressed in various tissues of the body. There are two subtypes of the receptor in humans, melatonin receptor 1 (MT 1) and melatonin receptor 2 (MT 2). [2] Melatonin and melatonin receptor agonists, on market or in clinical trials, all bind to and activate both receptor types. [1]
Melatonin receptors are G protein-coupled receptors (GPCR) which bind melatonin. [1] Three types of melatonin receptors have been cloned.The MT 1 (or Mel 1A or MTNR1A) and MT 2 (or Mel 1B or MTNR1B) receptor subtypes are present in humans and other mammals, [2] while an additional melatonin receptor subtype MT 3 (or Mel 1C or MTNR1C) has been identified in amphibia and birds. [3]
Melatonin may be useful in the treatment of delayed sleep phase syndrome. [9] Melatonin is known to reduce jet lag, especially in eastward travel. However, if it is not taken at the correct time, it can instead delay adaptation. [30] Melatonin appears to have limited use against the sleep problems of people who work shift work. [31]
It is the penultimate enzyme in the melatonin synthesis controlling the night/day rhythm in melatonin production in the vertebrate pineal gland. Melatonin is essential for seasonal reproduction, modulates the function of the circadian clock in the suprachiasmatic nucleus, and influences activity and sleep. Due to its important role in circadian ...
A small improvement in sleep onset and total sleep time by using melatonin has been shown in recent systematic reviews. [32] Synthetic melatonin, also known as melatonin receptor agonist, is also used for sleeping disorders by mimicking the action of melatonin. Examples are tasimelteon and ramelteon.