Caliendo G, Santagada V, Perissutti E, Fiorino F
Dipartimento di Chimica Farmaceutica e Tossicologica, Via D. Montesano, 49, Naples, Italy.
Curr Med Chem. 2005;12(15):1721-53. doi: 10.2174/0929867054367220.
Serotonin is a neuromediator, well-know for its implication in mood regulation, anxiety, depression and, insomnia as well as in normal human function such as sleep, sexual activity and appetite. In this way, serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists and pharmaceutical companies. Among 5-HTRs, the 5-HT1A subtype is the best studied, and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT1A receptor sites such as aminotetralins, ergolines, arylpiperazines, indolylalkylamines, aporphines and aryloxyalkyl-amines. In this review, we report an overview of the 5-HT1A receptor ligands, belonging to different chemical classes.
血清素是一种神经介质,因其在情绪调节、焦虑、抑郁、失眠以及睡眠、性活动和食欲等正常人体功能中的作用而广为人知。因此,血清素(5-羟色胺,5-HT)是药物化学家们和制药公司最感兴趣的靶点之一。在5-羟色胺受体(5-HTRs)中,5-HT1A亚型是研究得最为深入的,人们普遍认为它与焦虑和抑郁等精神疾病有关。已知有几种结构不同的化合物可与5-HT1A受体位点结合,如氨基四氢萘、麦角灵、芳基哌嗪、吲哚烷基胺、阿朴啡和芳氧基烷基胺。在本综述中,我们报告了属于不同化学类别的5-HT1A受体配体的概述。