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Loratadine and analogs: Discovery and preliminary SAR of inhibitors of the amino acid transporter B0AT2

Cuboni, Serena ; Devigny, Christian ; Hoogeland, Bastiaan ; Strasser, Andrea ; Pomplun, Sebastian ; Hauger, Barbara ; Höfner, Georg ; Wanner, Klaus ; Eder, Matthias ; Buschauer, Armin ; Holsboer, Florian ; Hausch, Felix


B0AT2, encoded by the SLC6A15 gene, is a transporter for neutral amino acids that has recently been implicated in mood and metabolic disorders. It is predominantly expressed in the brain but little is otherwise known about its function. In order to identify inhibitors for this transporter we screened a library of different 3133 bioactive compounds. Loratadine, a clinically used histamine H1 ...


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