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1. New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.

Author

Taliani S, Simorini F, Sergianni V, La Motta C, Da Settimo F, Cosimelli B, Abignente E, Greco G, Novellino E, Rossi L, Gremigni V, Spinetti F, Chelli B, and Martini C

Subjects
Animals, Brain metabolism, Cell Line, Tumor, Drug Design, Fluorescent Dyes chemistry, Fluorescent Dyes pharmacology, In Vitro Techniques, Indoles chemistry, Indoles pharmacology, Ligands, Radioligand Assay, Rats, Spectrophotometry, Ultraviolet, Fluorescent Dyes chemical synthesis, Indoles chemical synthesis, Receptors, GABA-A metabolism
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.

Published
2007
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