title: [Pharmacology of excitatory amino acid transporters (EAATs and VGLUTs)].
abstract: L-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS). It contributes not only to fast synaptic neurotransmission but also to complex physiological processes like plasticity, learning, and memory. Glutamate is synthesized in the cytoplasm and stored in synaptic vesicles by a proton gradient-dependent uptake system (VGLUTs). Following its exocytotic release, glutamate activates different kinds of glutamate receptors and mediates excitatory neurotransmission. To terminate the action of glutamate and maintain its extracellular concentration below excitotoxic levels, glutamate is quickly removed by Na(+)-dependent glutamate transporters (EAATs). Recently, three vesicular glutamate transporters (VGLUT1-3) and five Na(+)-dependent glutamate transporters (EAAT1-5) were identified. VGLUTs and EAATs are thought to play important roles in neuronal disorders, such as amyotrophic lateral sclerosis, Alzheimer's disease, cerebral ischemia, and Huntington's disease. In this review, the development of new compounds to regulate the function of VGLUTs and EAATs will be described.
authors.affiliation: National Institute of Advanced Industrial Science and Technology, Ikeda, Osaka, Japan. yasushi.shigeri@aist.go.jp
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Shigeri
authors.forename: Keiko
authors.initials: K
authors.lastname: Shimamoto
mesh_terms: D027322:Amino Acid Transport System X-AG / Q000737:chemistry / Q000235:genetics / Q000502:physiology*; D000818:Animals; D015195:Drug Design; D018698:Glutamic Acid / Q000378:metabolism* / Q000502:physiology; D006801:Humans; D007858:Learning; D008568:Memory; D019636:Neurodegenerative Diseases / Q000209:etiology; D009473:Neuronal Plasticity; D009435:Synaptic Transmission
chemical_list: D027322:Amino Acid Transport System X-AG; D018698:Glutamic Acid