| 翻訳と辞書 |
| Melatonin receptor agonist ： ウィキペディア英語版 |
Melatonin receptor agonist
Melatonin receptor agonists are analogues of melatonin that bind to and activate the melatonin receptor. Agonists of the melatonin receptor have a number of therapeutic applications including treatment of sleep disorders and depression. The discovery and development of melatonin receptor agonists was motivated by the need for more potent analogues than melatonin, with better pharmacokinetics and longer half-life. Melatonin receptor agonists were developed with the melatonin structure as a model.〔
The melatonin receptors are G protein-coupled receptors and are expressed in various tissues of the body. There are two subtypes of the receptor in humans, melatonin receptor 1 (MT1) and melatonin receptor 2 (MT2). Melatonin and melatonin receptor agonists, on market or in clinical trials, all bind to and activate both receptor types.〔 The binding of the agonists to the receptors has been investigated for over two decades or since 1986. It is somewhat known, but still not fully understood.〔 When melatonin receptor agonists bind to and activate their receptors it causes numerous physiological processes.〔〔
==History==
In 1917 McCord and Allen discovered melatonin itself. In 1958, Aaron B. Lerner and his colleagues isolated the substance N-acetyl-5-methoxytryptamine and named it melatonin.〔〔 High-affinity melatonin binding sites were pharmacologically characterized in the bovine brain in 1979. The first melatonergic receptor was cloned from melanophores of ''Xenopus laevis'' in the 1990s.〔 In 1994 the melatonin receptors were characterized and cloned in the human being.
TIK-301 (PD-6735, LY-156,735) has been in phase II clinical trial in the United States (US) since 2002.〔 The FDA granted TIK-301 orphan drug designation in May 2004, to use as a treatment for circadian rhythm sleep disorder in blind individuals without light perception and individuals with tardive dyskinesia.〔 In 2005 ramelteon (Rozerem®) was approved in the US indicated for treatment of insomnia, characterized as difficulty with falling asleep, in adults. Melatonin in the form of prolonged release (trade name Circadin®) was approved in 2007 in Europe (EU) for use as a short-term treatment, in patients 55 years or older, for primary insomnia (poor quality of sleep).〔http://www.ema.europa.eu〕 Products containing melatonin are available as a dietary supplement in the United States and Canada. In 2009 agomelatine (Valdoxan®, Melitor®, Thymanax®) was also approved in Europe and is indicated for the treatment of major depressive disorder in adults.〔 Tasimelteon completed the phase III clinical trial in the United States for primary insomnia in 2010. The Food and Drug Administration (FDA) granted tasimelteon orphan drug designation status for blind individuals without light perception with non-24-hour sleep–wake disorder in January the same year, and final FDA approval for the same purpose was achieved in January 2014 under the trade name Hetlioz®.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
■ウィキペディアで「Melatonin receptor agonist」の詳細全文を読む
スポンサード リンク
| 翻訳と辞書 : 翻訳のためのインターネットリソース |
Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.
|
|