New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
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.
Taliani
Sabrina
S
Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy. taliani@farm.unipi.it
Simorini
Francesca
F
Sergianni
Valentina
V
La Motta
Concettina
C
Da Settimo
Federico
F
Cosimelli
Barbara
B
Abignente
Enrico
E
Greco
Giovanni
G
Novellino
Ettore
E
Rossi
Leonardo
L
Gremigni
Vittorio
V
Spinetti
Francesca
F
Chelli
Beatrice
B
Martini
Claudia
C
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
D005456:Fluorescent Dyes; D007211:Indoles; D008024:Ligands; D011963:Receptors, GABA-A