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代谢型谷氨酸受体 5(mGluR5)正电子发射断层扫描(PET)成像用放射性配体。

Radioligands for the PET imaging of metabotropic glutamate receptor subtype 5 (mGluR5).

机构信息

Center for Radiopharmaceutical Sciences of ETH, PSI and USZ, Department of Chemistry and Applied Biosciences, ETH Zurich, 8093 Zurich, Switzerland.

出版信息

Curr Top Med Chem. 2010;10(15):1558-68. doi: 10.2174/156802610793176783.

Abstract

Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR), which activate intracellular secondary messenger systems when bound by the physiological ligand glutamate. Modulation of mGluR5s has potential for the treatment of variety of psychiatric and neurological diseases such as depression, anxiety, schizophrenia and Parkinson's disease. Positron emission tomography (PET) might offer the possibility to visualize the mGluR5 and present an interesting tool for studying this receptor-subtype under physiologic and pathologic conditions. In this review paper, emphasis is given to the radiosynthesis, in vitro and in vivo characterization of recently published mGluR5 PET tracers.

摘要

代谢型谷氨酸受体(mGluRs)是 G 蛋白偶联受体(GPCR),当与生理配体谷氨酸结合时,会激活细胞内的二级信使系统。mGluR5 的调节可能对治疗各种精神和神经疾病(如抑郁症、焦虑症、精神分裂症和帕金森病)具有潜在的作用。正电子发射断层扫描(PET)可能提供可视化 mGluR5 的可能性,并为在生理和病理条件下研究这种受体亚型提供一种有趣的工具。在这篇综述文章中,重点介绍了最近发表的 mGluR5 PET 示踪剂的放射合成、体外和体内特性。

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