同位素 ›› 2019, Vol. 32 ›› Issue (3): 218-230.DOI: 10.7538/tws.2019.32.03.0218

• 创刊30周年纪念专刊 • 上一篇    下一篇

中枢神经系统α7烟碱型乙酰神经胆碱受体显像剂研究进展

高航;张华北   

  1. 放射性药物教育部重点实验室 北京师范大学 化学学院,北京100875
  • 出版日期:2019-06-20 发布日期:2019-06-13

Research Progress of Radioligands for α7 Nicotinic Acetylcholine Receptor

GAO Hang;ZHANG Huabei   

  1. Key Laboratory of Radiopharmaceuticals, Ministry of Education,College of Chemistry, Beijing Normal University, Beijing 100875, China
  • Online:2019-06-20 Published:2019-06-13

摘要:

α7烟碱型乙酰神经胆碱受体(α7-nAChRs)与中枢神经系统多种功能和退行性神经疾病密切相关。正电子发射断层显像(PET)、单光子发射计算机化断层显像(SPECT)技术的发展,在分子水平为退行性神经疾病早期诊断提供了可能。研制出以α7 nAChR为靶点的亲和性高,特异性强,选择性好的显像剂对以老年痴呆为主的退行性神经疾病早期诊断和疗效检测具有重要意义。本文介绍了国内外α7 nAChRs放射性配体近几年发展状况,并简要介绍了各配体优缺点及未来展望。

关键词: 发射断层, AD, 显像剂, a7 nAChR

Abstract:

α7 nicotinic acetylcholine receptors (α7-nAChRs) are closely related to various functions of the central nervous system and degenerative neurological diseases. With the development of positron emission tomography (PET) and single photon emission computerized tomography (SPECT), it is possible to early diagnose neurodegenerative diseases at molecular level. It is of great significance to develop an imaging agent with high affinity, specificity and selectivity targeting α7-nAChR for the early diagnosis and therapeutic effect detection of degenerative neuropathy with Alzheimer's disease as the main target. In this paper, we summarized the development of a7 nAChR radioligands at home and abroad in recent years. The advantages, disadvantages and future prospects of these ligands are briefly introduced.

Key words: emission tomography, AD, imaging agent, α7 nAChR