MT1 and MT2 Melatonin Receptors: A Therapeutic Perspective.
MT1 and MT2 Melatonin Receptors: A Therapeutic Perspective.
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DOI：
10.1146/annurev-pharmtox-010814-124742
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发表时间：
2016
影响因子：
12.5
通讯作者：
Dubocovich ML
中科院分区：
文献类型：
--
作者：
Liu J;Clough SJ;Hutchinson AJ;Adamah-Biassi EB;Popovska-Gorevski M;Dubocovich ML
褪黑激素或5-甲氧基-N-乙酰色胺由松果体合成并释放，并在视网膜中局部遵循昼夜节律，白天水平低，晚上水平升高。褪黑激素激活两种高亲和力G蛋白偶联受体，称为MT 1和MT 2，在睡眠和昼夜节律异常，情绪障碍，学习和记忆，神经保护，药物滥用和癌症中发挥有益作用。在了解褪黑激素受体在调节睡眠和昼夜节律中的作用方面的进展已经导致发现了一类用于治疗失眠、昼夜节律、情绪障碍和癌症的新型褪黑激素激动剂。本文综述了缓释褪黑激素制剂的药理学性质（即，Circadin®）和合成配体（即，阿戈美拉汀、雷美琼、他司美琼），重点在于鉴定通过MT 1和MT 2受体活化介导的特异性治疗作用。靶向MT 1或MT 2褪黑激素受体的选择性配体的发现可以促进新的和更有效的治疗剂的开发。
Melatonin, or 5-methoxy-N-acetyltryptamine, is synthesized and released by the pineal gland and locally in the retina following a circadian rhythm, with low levels during the day and elevated levels at night. Melatonin activates two high-affinity G protein–coupled receptors, termed MT1 and MT2, to exert beneficial actions in sleep and circadian abnormality, mood disorders, learning and memory, neuroprotection, drug abuse, and cancer. Progress in understanding the role of melatonin receptors in the modulation of sleep and circadian rhythms has led to the discovery of a novel class of melatonin agonists for treating insomnia, circadian rhythms, mood disorders, and cancer. This review describes the pharmacological properties of a slow-release melatonin preparation (i.e., Circadin®) and synthetic ligands (i.e., agomelatine, ramelteon, tasimelteon), with emphasis on identifying specific therapeutic effects mediated through MT1 and MT2 receptor activation. Discovery of selective ligands targeting the MT1 or the MT2 melatonin receptors may promote the development of novel and more efficacious therapeutic agents.
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影响因子：
1.7
作者：
Al-Ghoul, WM;Herman, MD;Dubocovich, ML
通讯作者：
Dubocovich, ML
影响因子：
3.5
作者：
Adamah-Biassi EB;Hudson RL;Dubocovich ML
通讯作者：
Dubocovich ML
影响因子：
9.7
作者：
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通讯作者：
Hill, SM
影响因子：
3.5
作者：
Benloucif, S;Dubocovich, ML
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Dubocovich, ML
影响因子：
14
作者：
通讯作者：
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