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Beschreibung

A cell-permeable acryloylcarbamate compound that selectively targets the PDZ (PSD-95/Discs-large/ZO-1 homology) domain of PICK1 (protein interacting with C kinase 1), but not those of PSD-95 (postsynaptic density protein 95) and GRIP1 (glutamate receptor interacting protein 1), effectively competing against dopamine transporter/DAT (Ki ~10 µ,M), GluR2 (Ki ~10 µ,M), and mRluR7a, c-terminus binding to PICK1 PDZ. Shown to accelerate internalized GluR2 surface recycling and suppress both long-term depression and potentiation in rat and murine hippocampal neurons., A cell-permeable acryloylcarbamate compound that selectively targets the PDZ (PSD-95/Discs-large/ZO-1 homology) domain of PICK1 (protein interacting with C kinase 1), but not PDZ domains of PSD-95 (postsynaptic density protein 95) and GRIP1 (glutamate receptor interacting protein 1), effectively competing against dopamine transporter/DAT (Ki ~10 µ,M in competitive binding assays), GluR2 (Ki ~10 µ,M in competitive binding assays), and mRluR7a (~70% inhibition by Co-IP using lysates from 50 µ,M FSC231-treated HEK293), c-terminus binding to PICK1 PDZ. Shown to accelerate GluR2 surface recycling after NMDR-induced internalization (t1/2 = 7.5 vs 10 min with and without 50 µ,M FSC231 treatment) in rat hippocampal neurons and prevent both LTD (% long-term depression = 74 vs 50 with and without 50 µ,M FSC231 treatment) and LTP (% long-term potentiation = 137 vs 266 with and without 50 µ,M FSC231 treatment) in murine hippocampal slices.