| 外観 | 白色〜うすい褐色, 結晶〜粉末 |
| 溶解性 | 熱水、エタノール及びアセトンに溶ける。 |
| 解説 | メラトニン，融点116～118 ℃．淡黄色の板状晶．エタノールに可溶．ほ乳類では生殖器の発育を抑える作用があり，思春期になると血中濃度が急激に低下する．このほか，視交さ上核に作用し，生物時計(サーカディアンリズム)を調節していると考えられることから，時差ぼけの薬として市販されている．両生類ではメラニン細胞に作用し，メラニン顆粒の凝集を起こし，体色を薄くする． 森北出版「化学辞典（第2版）
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| 用途 | メラトニン（英: Melatonin）は、動物、植物、微生物に存在するホルモンであり、また化学的にN-アセチル-5-メトキシトリプタミン（N-acetyl-5-methoxytryptamine）として知られる。動物では、メラトニンの血中濃度は1日の周期で変化しており、それぞれの生物学的な機能における概日リズムによる同調を行っている。
メラトニンによる多くの生物学的な効果は、メラトニン受容体（英語版）の活性を通して生成され、他にも広範囲にわたる強力な抗酸化物質としての役割によって 特に核DNAやミトコンドリアDNAを保護する。 |
| 効能 | 抗けいれん薬, 脳保護薬, 催眠鎮静薬, メラトニン受容体作動薬 |
| 製造 | メラトニン，ほ乳類の松果体で，トリプトファンからセロトニンを経て合成されるホルモン． |
| 使用上の注意 | 不活性ガス封入 |
| 説明 | Melatonin, at times referred to as the “hormone of darkness,” normally is secreted during the night.
It is synthesized in the pineal gland, and its secretion is controlled by the suprachiasmatic nucleus, following an
endogenous circadian rhythm. Studies indicate that melatonin may |
| 化学的特性 | Off-White Powder |
| 天然物の起源 | Melatonin is a naturally occurring hormone in the body. |
| 使用 | Immunostimulant;Melatonin receptor ligand |
| 使用 | Hormone postulated to mediate photoperiodicity in mammals. Inhibits cerebellar nitric oxide synthetase |
| 使用 | Melatonin has complex effects on apoptotic pathways, inhibiting apoptosis in immune cells and neurons but enhancing apoptotic cell death of cancer cells. Inhibits proliferation/metastasis of breast cancer cells by inhibiting estrogen receptor action. |
| 使用 | Melatonine can be used in sleep induction, modifies circadian rhythm, antioxidant, free radical scavenger |
| 定義 | ChEBI: A member of the class of acetamides that is acetamide in which one of the hydrogens attached to the nitrogen atom is replaced by a 2-(5-methoxy-1H-indol-3-yl)ethyl group. It is a hormone secreted by the pineal gland in humans. |
| 世界保健機関（WHO） | Melatonin is promoted as a cure for travel sickness, jet-lag and
insomnia and has recently been claimed in the United States to reverse the ageing
process. A synthetic version has been freely available from health food shops and
pharmacies as a "nutritional supplement" since 1993. |
| 一般的な説明 | A hormone that has been postulated as being a mediator of photic-induced anti-gonadotropic activity in photoperiodic mammals. Counteracts the apoptotic effects of etoposide in bone marrow cells. Melatonin receptors are coupled to a G-protein system. Inhibits rat cerebellar nitric oxide synthase (NOS). |
| 生物活性 | Endogenous hormone that acts as an agonist at melatonin receptors MT 1 and MT 2 . Exhibits a prominent role in the control of circadian rhythm, displays immunomodulatory activity and acts as a powerful antioxidant in vivo . |
| Biochem/physiol Actions | Hormone; mediates photoperiodicity in mammals; inhibits cerebellar nitric oxide synthetase; peroxynitrite scavenger. Melatonin has complex effects on apoptotic pathways, inhibiting apoptosis in immune cells and neurons but enhancing apoptotic cell death of cancer cells. Inhibits proliferation/metastasis of breast cancer cells by inhibiting estrogen receptor action. |
| 臨床応用 | Melatonin is most effective in young individuals and appears to be less effective in elderly individuals (possibly because of a decreased number of receptors). Melatonin causes a phase shift of approximately 1 hour per day. This means that the use of melatonin in the morning can delay the onset of evening sleepiness, whereas melatonin taken in the evening has been associated with faster onset of sleep and increased total sleep time. Melatonin is sold as a food supplement in the United States, but it has become popular for use as a hypnotic and for alleviating jet lag (a flight across five or more time zones) and helping to resynchronize individuals who have difficulty adapting to night-shift work. have effects on circadian rhythm and sleep processes. The presence of a pharmacologically specific receptor for melatonin in which the molecular structure is known are referred to as MT1, MT2, and MT3 receptors. The MT1 and MT2 receptors are high-affinity G protein coupled receptors, whereas MT3 is a form of quinone reductase. The MT1 receptor appears to be primarily involved in initiating sleep, whereas the MT2 receptor appears to mediate melatonins effect in the eye, circadian rhythm, and vascular effects. The importance of MT3, although widely distributed in different tissues, is currently unknown. The normal physiological concentration of melatonin observed at night is approximately 100 to 200 pg/mL, and oral doses of 0.1 to 0.3 mg of melatonin are adequate to obtain these concentrations even though melatonin frequently is given at doses of 1 to 10 mg to obtain supraphysiological levels. These higher doses may be the reason for some of the side effects not currently associated with the melatonin receptors. |
| Veterinary Drugs and Treatments | Melatonin may be useful to treat Alopecia-X in Nordic breeds, canine
pattern baldness, or canine recurrent flank alopecia in dogs.
It has been used anecdotally for the treatment of sleep cycle disorders
in cats and geriatric dogs and to treat phobias and separation
anxiety in dogs. Melatonin implants are used in the mink and fox
pelt industries to promote the development of luxurious hair coats.
Implants are also used to improve early breeding and ovulation
rates in sheep and goats. Preliminary research is being done for this
purpose in horses also.
In pigs, one study (Bubenik, Ayles et al. 1998) demonstrated that
5 mg/kg in feed reduced the incidence
of gastric ulcers in young
pigs. |
| 貯蔵 | Store at -20°C |