title: Synthesis, radiolabeling and baboon SPECT imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl)tropane ([(123)I]YP256) as a serotonin transporter radiotracer.
abstract: To develop a potential SPECT probe to evaluate the integrity of the serotoninergic system (5-HTT) whose dysfunction is linked to several disease conditions such as Parkinson's disease, Alzheimer's disease and depression, we report the synthesis, radiolabeling and in vivo baboon imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl) tropane (YP256, 6). The radiolabeling was performed by iododestannylation using sodium [(123)I]iodide and peracetic acid. Although the ligand displayed high selectivity for 5-HTT over dopamine transporter in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo.
authors.affiliation: Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA.
authors.forename: Frederic
authors.initials: F
authors.lastname: Bois
authors.forename: Ronald M
authors.initials: RM
authors.lastname: Baldwin
authors.forename: Louis
authors.initials: L
authors.lastname: Amici
authors.forename: Mohammed S
authors.initials: MS
authors.lastname: Al-Tikriti
authors.forename: Nora
authors.initials: N
authors.lastname: Kula
authors.forename: Ross
authors.initials: R
authors.lastname: Baldessarini
authors.forename: Robert B
authors.initials: RB
authors.lastname: Innis
authors.forename: Julie K
authors.initials: JK
authors.lastname: Staley
authors.forename: Gilles D
authors.initials: GD
authors.lastname: Tamagnan
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003042:Cocaine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D005260:Female; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D010215:Papio; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: C528135:2-carbomethoxy-3-(3'-iodophenyl)tropane; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D050486:Serotonin Plasma Membrane Transport Proteins; D003042:Cocaine