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• W2037819091 abstract "Melatonin has been used successfully to treat insomnia, but has not received regulatory approval by the FDA because it can be sold freely as a food supplement. This has prompted a search by pharmaceutical companies for patentable melatonin receptor ligands, and the melatonin receptor agonist ramelteon has received particular attention. This Review describes the pharmacology and metabolism of ramelteon, assesses evidence from animal models and clinical studies that supports its efficacy in treating insomnia, and discusses its possible mechanism of action. Melatonin, a chronobiotic that participates in the control of the circadian system, is known for its sleep-promoting effects, which include shortening of sleep latency and lengthening of sleep duration. As a result of its short half-life, melatonin does not exhibit undesirable side effects, and its broad applicability for a variety of sleep problems has been the focus of numerous scientific studies. Melatonin has not, however, received regulatory approval from the US FDA as a drug, because it can be sold freely as a food supplement. Consequently, there has been an active search for patentable melatonin receptor ligands in recent years. Ramelteon, an agonist that acts solely on melatonin MT1 and MT2 receptors, is of particular interest, and preliminary research indicates that it holds considerable promise for clinical applications. Ramelteon has been shown to induce sleep initiation and maintenance in various animal models and in clinical trials. In chronic insomnia, ramelteon decreases sleep latency and increases total sleep time and sleep efficiency, without causing hangover, addiction or withdrawal effects. Ramelteon is thought to promote sleep by influencing homeostatic sleep signaling mediated by the suprachiasmatic nucleus. Although ramelteon's metabolism and pharmacokinetics differ from those of melatonin, its safety seems to be sufficient for short-term application. Its long-term effects remain to be determined." @default.
• W2037819091 created "2016-06-24" @default.
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• W2037819091 date "2007-04-01" @default.
• W2037819091 modified "2023-10-02" @default.
• W2037819091 title "Drug Insight: the use of melatonergic agonists for the treatment of insomnia—focus on ramelteon" @default.
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• W2037819091 doi "https://doi.org/10.1038/ncpneuro0467" @default.
• W2037819091 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17410109" @default.
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