title: New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy. taliani@farm.unipi.it
authors.forename: Sabrina
authors.initials: S
authors.lastname: Taliani
authors.forename: Francesca
authors.initials: F
authors.lastname: Simorini
authors.forename: Valentina
authors.initials: V
authors.lastname: Sergianni
authors.forename: Concettina
authors.initials: C
authors.lastname: La Motta
authors.forename: Federico
authors.initials: F
authors.lastname: Da Settimo
authors.forename: Barbara
authors.initials: B
authors.lastname: Cosimelli
authors.forename: Enrico
authors.initials: E
authors.lastname: Abignente
authors.forename: Giovanni
authors.initials: G
authors.lastname: Greco
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Leonardo
authors.initials: L
authors.lastname: Rossi
authors.forename: Vittorio
authors.initials: V
authors.lastname: Gremigni
authors.forename: Francesca
authors.initials: F
authors.lastname: Spinetti
authors.forename: Beatrice
authors.initials: B
authors.lastname: Chelli
authors.forename: Claudia
authors.initials: C
authors.lastname: Martini
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D045744:Cell Line, Tumor; D015195:Drug Design; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D011869:Radioligand Assay; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D013056:Spectrophotometry, Ultraviolet
chemical_list: D005456:Fluorescent Dyes; D007211:Indoles; D008024:Ligands; D011963:Receptors, GABA-A