title: Synthesis and in vitro binding properties of halogenated analogues of GBR as new dopamine uptake carrier ligands.
abstract: We present the original synthesis of two halogenated analogues of the diphenyl piperazine GBR, bromo-GBR and iodo-GBR, as new dopamine uptake carrier ligands. The derivatives were purified by HPLC and chemically characterized. Bromo-GBR and iodo-GBR and iodo-GBR are potent inhibitors of [3H]GBR 12935 binding to rat striatal membrane, with Ki values of 116 and 113 nM, respectively. We prepared iodo-GBR labeled with iodide-125 from the brominated derivative and concluded that [123I]iodo-GBR could be a potential tool to explore the in vivo dopamine uptake carrier.
authors.affiliation: INSERM U 316, Tours, France.
authors.forename: C
authors.initials: C
authors.lastname: Foulon
authors.forename: L
authors.initials: L
authors.lastname: Garreau
authors.forename: S
authors.initials: S
authors.lastname: Chalon
authors.forename: G
authors.initials: G
authors.lastname: Desplanches
authors.forename: Y
authors.initials: Y
authors.lastname: Frangin
authors.forename: J C
authors.initials: JC
authors.lastname: Besnard
authors.forename: J L
authors.initials: JL
authors.lastname: Baulieu
authors.forename: D
authors.initials: D
authors.lastname: Guilloteau
mesh_terms: D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D001967:Bromine Radioisotopes; D004298:Dopamine / Q000378:metabolism*; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D008024:Ligands; D010879:Piperazines / Q000138:chemical synthesis* / Q000378:metabolism; D011877:Radionuclide Imaging; D051381:Rats
chemical_list: D001967:Bromine Radioisotopes; D007457:Iodine Radioisotopes; D008024:Ligands; D010879:Piperazines; C076872:4-iodo-GBR; C076874:4-bromo-GBR; D004298:Dopamine