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- W2912583212 abstract "Cerebral edema in ischemic stroke can lead to increased intracranial pressure, reduced cerebral blood flow and neuronal death. Unfortunately, current therapies for cerebral edema are either ineffective or highly invasive. During the development of cytotoxic and subsequent ionic cerebral edema water enters the brain by moving across an intact blood brain barrier and through aquaporin-4 (AQP4) at astrocyte endfeet. Using AQP4-expressing cells, we screened small molecule libraries for inhibitors that reduce AQP4-mediated water permeability. Additional functional assays were used to validate AQP4 inhibition and identified a promising structural series for medicinal chemistry. These efforts improved potency and revealed a compound we designated AER-270, N-[3,5-bis (trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide. AER-270 and a prodrug with enhanced solubility, AER-271 2-{[3,5-Bis(trifluoromethyl) phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, improved neurological outcome and reduced swelling in two models of CNS injury complicated by cerebral edema: water intoxication and ischemic stroke modeled by middle cerebral artery occlusion." @default.
- W2912583212 created "2019-02-21" @default.
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- W2912583212 date "2019-04-01" @default.
- W2912583212 modified "2023-10-15" @default.
- W2912583212 title "Functionalized Phenylbenzamides Inhibit Aquaporin-4 Reducing Cerebral Edema and Improving Outcome in Two Models of CNS Injury" @default.
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- W2912583212 doi "https://doi.org/10.1016/j.neuroscience.2019.01.034" @default.
- W2912583212 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6495193" @default.
- W2912583212 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30738082" @default.
- W2912583212 hasPublicationYear "2019" @default.
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