CERMEP-Imaging Platform, University Hospital of Lyon (Hospices Civils de Lyon), 59 Boulevard Pinel, F-69003 Lyon, France.
Curr Med Chem. 2014;21(1):70-81. doi: 10.2174/09298673113209990215.
Serotonin and its various receptors are involved in numerous brain functions and neuropsychiatric disorders. The 5-HT1A family is the best characterized subtype of the fourteen currently known 5-HT receptors. The 5-HT1A receptor is closely involved in the pathogenesis of anxiety, depression, epilepsy and eating disorders and therefore is an important target for drug therapy. The development in the 1980s of molecules specifically targeting this receptor was followed by the rapid development of corresponding PET neuroimaging. Because this receptor represents a crucial target in neuroscience, a large number of radioligands have been developed by academic and industry centers for visualization and quantification, first in living animals and ultimately in humans. After a brief account of some of the structural and functional characteristics of brain 5-HT1A receptors, this review focuses on the main lines of evolution opened up by preclinical and clinical 5-HT1A PET radiopharmaceuticals, illustrating the potential value of PET for clinical research and drug development.
血清素及其各种受体参与许多大脑功能和神经精神疾病。5-HT1A 家族是目前已知的 14 种 5-HT 受体中研究得最充分的亚型。5-HT1A 受体与焦虑、抑郁、癫痫和进食障碍的发病机制密切相关，因此是药物治疗的重要靶点。上世纪 80 年代专门针对该受体的分子的发展，随后是相应的正电子发射断层扫描（PET）神经影像学的快速发展。由于该受体代表了神经科学中的一个关键靶点，因此学术界和工业界的研究中心开发了大量用于可视化和定量的放射性配体，首先是在活体动物中，最终是在人类中。本文简要介绍了大脑 5-HT1A 受体的一些结构和功能特征，重点介绍了临床前和临床 5-HT1A PET 放射性药物所开辟的主要发展方向，说明了 PET 在临床研究和药物开发方面的潜在价值。
