Odile Poirel, Lauren E Mamer, Melissa A Herman, Marie Arnulf-Kempcke, Myriam Kervern, Brigitte Potier, Stephanie Miot, Jing Wang, Franck-Cyril Favre-Besse, Isabelle Brabet, Younès Laras, Hugues-Olivier Bertrand, Francine Acher, Jean-Philippe Pin, Jean-Luc Puel, Bruno Giros, Jacques Epelbaum, Christian Rosenmund, Patrick Dutar, Stephanie Daumas, Salah El Mestikawy, Nicolas Pietrancosta
Vesicular glutamate transporters (VGLUT1-3) mediate the uptake of glutamate into synaptic vesicles. VGLUTs are pivotal actors of excitatory transmission and of almost all brain functions. Their implication in various pathologies has been clearly documented. Despite their functional importance, the pharmacology of VGLUTs is limited to a few dyes such as Trypan Blue, Rose Bengal or Brilliant Yellow type. Here, we report the design and evaluation of new potent analogs based on Trypan Blue scaffold. Our best compound, named LSP5-2157, has an EC50 of 50 nM on glutamate vesicular uptake...
December 4, 2019: Neuropharmacology