title: Development of PET and SPECT probes for glutamate receptors.
abstract: 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.
authors: Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
authors: Takeshi
authors: 0000-0001-8141-1212
authors: T
authors: Fuchigami
authors: Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
authors: Morio
authors: M
authors: Nakayama
authors: Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
authors: Sakura
authors: 0000-0002-5198-4711
authors: S
authors: Yoshida
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D055808:Drug Discovery / Q000379:methods / Q000639:trends; D005456:Fluorescent Dyes / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D049268:Positron-Emission Tomography / Q000379:methods* / Q000639:trends; D017470:Receptors, Glutamate / Q000378:metabolism; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods* / Q000639:trends
chemical_list: D005456:Fluorescent Dyes; D017470:Receptors, Glutamate