Melatonin: Pharmacological Aspects and Clinical Trends

Melatonin: Pharmacological Aspects and Clinical Trends
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褪黑激素:药理学方面和临床趋势

DOI:
10.3109/00207454.2010.492921
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发表时间:
2010
影响因子:
2.2
通讯作者:
M. Fonteles
M. Fonteles
中科院分区:
医学4区
文献类型:
--
作者:
E. Rios;E. T. Venâncio;N. Rocha;D. Woods;S. Vasconcelos;D. Macêdo;F. Sousa;M. Fonteles

文献摘要

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摘要褪黑激素,即N-乙酰基-5-甲氧基色胺,是松果体在光/暗周期影响下产生的主要激素,已被证明具有大量的治疗可能性。它已在几个国家用于治疗盲人和轮班工人的昼夜节律紊乱、睡眠障碍、时差和睡眠-觉醒周期紊乱。在我们的作用机制中,Gi蛋白偶联的代谢型褪黑激素受体MT 1和MT 2是褪黑激素生理作用的主要介质。这种激素在生理和神经内分泌功能的调节中起着重要作用,例如季节性生殖节律的同步和昼夜节律周期的诱导。除其时间生物学作用外,已报道褪黑激素在哺乳动物中的几种药理学作用,包括镇静、抗氧化、抗焦虑、抗抑郁、抗惊厥和镇痛活性。有一些来自临床试验的证据表明,褪黑激素可以在这种情况下有所帮助。本文综述了褪黑激素药理作用的研究进展,指出了褪黑激素在神经退行性疾病和肿瘤性疾病治疗中的应用。褪黑激素的这些作用和用途被提及,但其中大多数需要进一步的验证性研究。
ABSTRACT Melatonin, N-acetyl-5-methoxytryptamine, the major hormone produced by the pineal gland under the influence of the dark/light cycle, has been shown to have a large number of therapeutic possibilities. It has been utilized in several countries for circadian rhythm disorders, sleep disturbances, jet lag, and sleep–wake cycle disturbances in blind people, and shift workers. In our mechanism of act, the Gi protein-coupled metabotropic melatonin receptors MT1 and MT2 are the primary mediators of the physiological actions of melatonin. This hormone plays an important role in the regulation of physiological and neuroendocrine functions, such as synchronization of seasonal reproductive rhythms and entrainment of circadian cycles. In addition to its chronobiological role, several pharmacological effects of melatonin have been reported in mammals including sedative, antioxidant, anxiolytic, antidepressant, anticonvulsant, and analgesic activities. There is some evidence from clinical trials that melatonin can be helpful in that event. Current trends of pharmacological functions of melatonin pointed out its use in the treatment of neurodegenerative and neoplastic diseases. These effects and uses of melatonin are mentioned but further confirmatory studies are needed in most of them.