Article ; Online: Design and Characterization of Prodrug-like Inhibitors for Preventing Glutamate Efflux through Reverse Transport.
ACS chemical neuroscience
2023 Volume 14, Issue 23, Page(s) 4252–4263
Abstract: Glutamate transporters are responsible for active transport of the major excitatory neurotransmitter glutamate across the cell membrane, regulating the extracellular glutamate concentration in the mammalian brain. Extracellular glutamate levels in the ... ...
| Abstract | Glutamate transporters are responsible for active transport of the major excitatory neurotransmitter glutamate across the cell membrane, regulating the extracellular glutamate concentration in the mammalian brain. Extracellular glutamate levels in the brain are usually in the submicromolar range but can increase by exocytosis, inhibition of cellular uptake, or through glutamate release by reverse transport, as well as other mechanisms, which can lead to neurodegeneration and neuronal cell death. Such conditions can be encountered upon energy deprivation during an ischemic stroke. Here, we developed acetoxymethyl (AM) ester prodrug-like derivatives of excitatory amino acid transporter (EAAT) inhibitors that permeate the cell membrane and are activated, most likely through hydrolysis by endogenous cellular esterases, to form the active EAAT inhibitor. Upon increase in external K |
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| MeSH term(s) | Animals ; Humans ; Glutamic Acid/metabolism ; Prodrugs/pharmacology ; Biological Transport ; Amino Acid Transport System X-AG/metabolism ; Esters ; Mammals/metabolism |
| Chemical Substances | Glutamic Acid (3KX376GY7L) ; Prodrugs ; Amino Acid Transport System X-AG ; Esters |
| Language | English |
| Publishing date | 2023-11-23 |
| Publishing country | United States |
| Document type | Journal Article ; Research Support, N.I.H., Extramural |
| ISSN | 1948-7193 |
| ISSN (online) | 1948-7193 |
| DOI | 10.1021/acschemneuro.3c00651 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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