| [image] [image] Melatonin | |
| 5-methoxy-N-acetyltryptamine | |
| Empiric formula | C13H16N2O2 |
| Molecular weight | 232.28 |
| Bioavailability | 30 - 50% |
| Metabolism | Liver |
| Elimination half life | 32 - 40 minutes |
| Excretion | Urine |
| Pregnancy category | ? |
| Delivery | 1mg, 2.5mg, 3mg, and 5mg capsules; 1mg/mL or 1mg/4mL liquid; .5mg and 3mg lozenges; 2.5mg sublingual tablets; 1mg, 2mg, and 3mg timed-release tablets |
| Indicated for: | |
Melatonin produced in the pineal gland acts as an endocrine hormone since it is released into the blood. On the other hand, melatonin produced by the retina and the GI tract is considered a paracrine hormone.
Melatonin helps regulate sleep-wake or circadian rhythms. Normally, production of melatonin by the pineal gland is stimulated by darkness and inhibited by light. Melatonin can suppress libido by inhibiting secretion of Luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the Anterior pituitary gland -- especially in mammals that have a Breeding season when daylight hours are long, such as Sheep. Nobel Prize laureate Julius Axelrod performed many of the seminal experiments elucidating the role of melatonin and the pineal gland in circadian rhythms. Beta blockers decrease nocturnal melatonin release.
Melatonin is synthesized by various plants such as rice and ingested melatonin was shown to be capable of reaching and binding to melatonin binding sites in the brain of mammals .
In recent times, melatonin has become available as a Drug and a Dietary supplement. It appears to have some use against Insomnia, Jet lag, and circadian misalignment. Melatonin is a powerful Antioxidant which can easily cross cell membranes including the Blood-brain barrier. It has been studied for the treatment of Cancer, immune disorders, cardiovascular diseases, depression, Seasonal affective disorder, and Sexual dysfunction; the results of most of these studies remain inconclusive. However, it has been shown to clearly ameliorate Seasonal affective disorder and circadian misalignment, in studies by Alfred J. Lewy (OHSU) and other researchers.
Melatonin is referred to by some biochemists and human physiologists as the master hormone, because it regulates the production of most human hormones, both paracrine and endocrine. In addition, melatonin, taken alone, is an immunoregulator that enhances T cell production somewhat. However, when melatonin is taken in conjunction with calcium, it is a very potent Immunostimulator of the T cell response. This is the reason it is used as an Adjuvant in many clinical protocols. Because it does not have to be prescribed, and since it is in the public domain, few doctors care to publicize its advantages. For the same reason, few clinical trials have been done to see its effectiveness in treating various diseases, such as cancer, obesity, HIV infection, and others.
To synthesize melatonin, serotonin is converted to N-acetylserotonin by the Enzyme 5-HT N-acetyltransferase. N-acetylserotonin is then converted to melatonin by the enzyme 5-hydroxyindole-O-methyltransferase. See Serotonin for details on how tryptophan is converted to serotonin.
Melatonin has been also shown to be a possible treatment of Alzheimer's Disease. It prevents the Hyper Phosphorlation of the protein TAU. TAU is a cytoskeletal protein that when hyperphosphorylated begins to clump up. As TAU clumps up it can no longer support the microtubules inside a dendrite or axon and the neurite begins to degrade. Melatonin has been shown to prevent this and could be a possible preventive cure for Alzheimer's disease. (Prevention of isoproterenol-induced hyperphosphorylation by melatonin in the rat) Acta Physilogica Sinica, February 25, 2005, 57 (1):7-12 ()
Melatonin has been shown to increase the lifespan of mice by 20% in some studies . This may be due to melatonin's ability to scavenge free radicals. Unlike other antioxidants, melatonin does not undergo Redox cycling. Redox cycling refers to the ability of a molecule to undergo reduction and oxidation repeatedly. This back-and-forth activity may allow other antioxidants (such as Vitamin C) to act as pro-oxidants, promoting free radical formation. However, once melatonin is oxidized, it cannot be reduced back to its former state because it forms several stable end-products upon reacting with free radicals. Therefore, it has been referred to as a terminal (or suicidal) antioxidant.
Other studies have noted that wearing garments such as bras are linked to a decrease in melatonin production.
| Tryptamines |
|---|
| 4-Acetoxy-DET | 4-Acetoxy-DIPT | 5-MeO-AMT | 5-MeO-DALT | 5-MeO-DET | 5-MeO-DIPT | 5-MeO-DMT | 5-MeO-MIPT | AET | AMT | Baeocystin | Bufotenin | DET | DIPT | DMT | DPT | Ethocin | Ibogaine | Iprocin | Miprocin | Melatonin | Norbaeocystin | Psilocin | Psilocybin | Rizatriptan | Serotonin | Sumatriptan | Tryptamine | Tryptophan |