Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3.


Screening a library of small-molecule compounds using a cell line expressing human GABA transporter 3 (hGAT3) in a [(3)H]GABA uptake assay identified isatin derivatives as a new class of hGAT3 inhibitors. A subsequent structure-activity relationship (SAR) study led to the identification of hGAT3-selective inhibitors (i.e., compounds 20 and 34) that were… (More)
DOI: 10.1021/acschemneuro.5b00150


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