Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders.
Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders.
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DOI：
10.1016/j.pharmthera.2010.08.013
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发表时间：
2011-02
影响因子：
13.5
通讯作者：
Hedlund, Peter B.
中科院分区：
文献类型：
--
作者：
Leopoldo, Marcello;Lacivita, Enza;Berardi, Francesco;Perrone, Roberto;Hedlund, Peter B.
关键词：
自从20世纪40年代在血清、哺乳动物肠粘膜和中枢神经系统中发现5-羟色胺（5-HT）以来，5-HT已被证明参与几乎所有的人类认知和行为功能，并且其神经化学的改变已被牵连到大量神经精神障碍的病因学中。5-HT受体亚型的克隆对于将其分类为由特定基因编码的特定蛋白分子具有重要意义。5-HT 7受体是最近分类的5-羟色胺受体家族的成员。自从它被发现以来，由于它存在于大脑功能相关区域，它一直是人们深入研究的对象。一些选择性拮抗剂和激动剂的可用性，与缺乏5-HT 7受体的转基因小鼠相结合，使人们能够更好地了解这种受体的病理生理作用。本文综述了5-HT 7受体的定位和药理学性质的数据，并总结了旨在发现选择性5-HT 7受体配体的构效关系研究结果。此外，概述了5-HT 7受体激动剂和拮抗剂在中枢神经系统疾病中的潜在治疗应用。
Since its discovery in the 1940s in serum, the mammalian intestinal mucosa, and in the central nervous system, serotonin (5-HT) has been shown to be involved in virtually all cognitive and behavioral human functions, and alterations in its neurochemistry have been implicated in the etiology of a plethora of neuropsychiatric disorders. The cloning of 5-HT receptor subtypes has been of importance in enabling them to be classified as specific protein molecules encoded by specific genes. The 5-HT7 receptor is the most recently classified member of the serotonin receptor family. Since its identification, it has been the subject of intense research efforts driven by its presence in functionally relevant regions of the brain. The availability of some selective antagonists and agonists, in combination with genetically modified mice lacking the 5-HT7 receptor, has allowed for a better understanding of the pathophysiological role of this receptor. This paper reviews data on localization and pharmacological properties of the 5-HT7 receptor, and summarizes the results of structure-activity relationship studies aimed at the discovery of selective 5-HT7 receptor ligands. Additionally, an overview of the potential therapeutic applications of 5-HT7 receptor agonists and antagonists in central nervous system disorders is presented.
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