Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders

被引：166

作者：

Leopoldo, Marcello ^{[1
]}

Lacivita, Enza ^{[1
]}

Berardi, Francesco ^{[1
]}

Perrone, Roberto ^{[1
]}

Hedlund, Peter B. ^{[2
]}

机构：

[1] Univ Bari A Moro, Dipartimento Farmacochim, I-70125 Bari, Italy

[2] Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA

来源：

PHARMACOLOGY & THERAPEUTICS | 2011年 / 129卷 / 02期

关键词：

Serotonin; 5-HT7; receptor; G-protein-coupled receptors; Structure-activity relationships; Depression; Anxiety; Circadian rhythm; IN-SITU HYBRIDIZATION; DORSAL RAPHE NUCLEUS; CHRONIC ANTIDEPRESSANT TREATMENT; OBSESSIVE-COMPULSIVE DISORDER; PROTEIN-COUPLED RECEPTORS; MAJOR DEPRESSIVE DISORDER; NOVELTY-SEEKING BEHAVIOR; MIDDLE MENINGEAL ARTERY; RAT PREFRONTAL CORTEX; FORCED SWIMMING TEST;

D O I：

10.1016/j.pharmthera.2010.08.013

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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. (C) 2010 Elsevier Inc. All rights reserved.

引用

页码：120 / 148

页数：29

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