- New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
Journal of medicinal chemistry (2007-01-19)
Sabrina Taliani, Francesca Simorini, Valentina Sergianni, Concettina La Motta, Federico Da Settimo, Barbara Cosimelli, Enrico Abignente, Giovanni Greco, Ettore Novellino, Leonardo Rossi, Vittorio Gremigni, Francesca Spinetti, Beatrice Chelli, Claudia Martini
PMID17228885
ABSTRACT
Fluorescent ligands for the peripheral-type benzodiazepine receptor (PBR) featuring the 7-nitrobenz-2-oxa-1,3-diazol-4-yl moiety were synthesized, based on N,N-dialkyl-2-phenylindol-3-ylglyoxylamides, a potent, selective class of PBR ligands previously described by us. All the new ligands are moderately to highly potent at the PBR, with a complete selectivity over the central benzodiazepine receptor. Results from fluorescence microscopy showed that these probes specifically labeled the PBR at the mitochondrial level in C6 glioma cells.
MATERIALS