Vesicular Glutamate Transporter Inhibitors: Structurally Modified Brilliant Yellow Analogs
| Autor: | J. Christian Althaus, Michael A. Sutton, Tetsufumi Ueda, Jason Kehrl, H. D. Hollis Showalter, Di Andra M. Rudzinski |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Nervous system Biology Neurotransmission Inhibitory postsynaptic potential Biochemistry Synaptic vesicle PC12 Cells 03 medical and health sciences Cellular and Molecular Neuroscience chemistry.chemical_compound 0302 clinical medicine Vesicular Glutamate Transport Proteins Molecular modification medicine Animals Cytotoxicity Brain Chemistry Benzenesulfonates Glutamate receptor Brain General Medicine Rats 030104 developmental biology medicine.anatomical_structure chemistry Synaptic Vesicles Azo Compounds 030217 neurology & neurosurgery Function (biology) |
| Zdroj: | Neurochemical research. 42(6) |
| ISSN: | 1573-6903 |
| Popis: | Glutamate uptake into synaptic vesicles in nerve terminals is a pivotal step in glutamate synaptic transmission. Glutamate is the major excitatory neurotransmitter and, as such, the vesicular glutamate transporter (VGLUT) responsible for this uptake is involved in a variety of nervous system functions and various types of pathophysiology. As yet, no VGLUT-specific, membrane-permeable agents have been developed to affect neuronal function in intact neurons, although two potent VGLUTspecific inhibitors are known. These compounds contain diazo and highly charged sulfonic acid groups, rendering them membrane-impermeable and potentially cytotoxic. In an effort to eliminate these undesirable properties, we have developed two novel agents, Brilliant Yellow analogs 1 and 2, which are free of these two groups. We show here that these agents retain highly VGLUT-selective inhibitory activity, despite their reduction in potency, and exhibit no significant cellular toxicity. Potential use of this molecular modification is discussed. |
| Databáze: | OpenAIRE |
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