Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.
Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.
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DOI：
10.2174/1568026616666160315142457
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发表时间：
2016
影响因子：
3.4
通讯作者：
Liang SH
中科院分区：
文献类型：
--
作者：
Kassenbrock A;Vasdev N;Liang SH
离子通道相关受体的正电子发射断层扫描（PET）神经成像是临床前和临床研究的一个发展中领域。本文综述了近年来神经精神药物研究中的三种受体的放射化学、临床前和临床PET成像研究进展：γ-氨基丁酸-苯二氮杂环己基（GABA）受体、烟碱乙酰胆碱受体（nAChR）和N-甲基-d-天冬氨酸（NMDA）受体。最近的努力，开发新的PET放射性配体，这些目标与改善脑摄取，选择性，稳定性和药代动力学的突出显示。
Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-d-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.