Fuchigami Takeshi, Nakayama Morio, Yoshida Sakura
Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
ScientificWorldJournal. 2015;2015:716514. doi: 10.1155/2015/716514. Epub 2015 Mar 22.
L-glutamate and its receptors (GluRs) play a key role in excitatory neurotransmission within the mammalian central nervous system (CNS). Impaired regulation of GluRs has also been implicated in various neurological disorders. GluRs are classified into two major groups: ionotropic GluRs (iGluRs), which are ligand-gated ion channels, and metabotropic GluRs (mGluRs), which are coupled to heterotrimeric guanosine nucleotide binding proteins (G-proteins). Positron emission tomography (PET) and single photon emission computed tomography (SPECT) imaging of GluRs could provide a novel view of CNS function and of a range of brain disorders, potentially leading to the development of new drug therapies. Although no satisfactory imaging agents have yet been developed for iGluRs, several PET ligands for mGluRs have been successfully employed in clinical studies. This paper reviews current progress towards the development of PET and SPECT probes for GluRs.
L-谷氨酸及其受体（GluRs）在哺乳动物中枢神经系统（CNS）的兴奋性神经传递中起关键作用。GluRs调节受损也与多种神经系统疾病有关。GluRs分为两大类：离子型谷氨酸受体（iGluRs），它们是配体门控离子通道；代谢型谷氨酸受体（mGluRs），它们与异三聚体鸟苷酸结合蛋白（G蛋白）偶联。对GluRs进行正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）成像可以为CNS功能以及一系列脑部疾病提供新的视角，有可能推动新药疗法的开发。尽管尚未开发出用于iGluRs的令人满意的成像剂，但几种用于mGluRs的PET配体已成功用于临床研究。本文综述了开发用于GluRs的PET和SPECT探针的当前进展。
