title: Radiosynthesis and biological evaluation of a promising sigma(2)-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer.
abstract: Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity sigma(2) receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [(18)F]3 and [(125)I]3, respectively. Studies of [(125)I]3 using murine 66 breast tumor membrane homogenates and evaluation of [(18)F]3 and [(125)I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging sigma(2) receptors in breast cancer.
authors.affiliation: Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 South Kingshighway Blvd., St. Louis, MO 63110, USA.
authors.forename: Zhude
authors.initials: Z
authors.lastname: Tu
authors.forename: Jinbin
authors.initials: J
authors.lastname: Xu
authors.forename: Lynne A
authors.initials: LA
authors.lastname: Jones
authors.forename: Shihong
authors.initials: S
authors.lastname: Li
authors.forename: Dexing
authors.initials: D
authors.lastname: Zeng
authors.forename: Mei-Ping
authors.initials: MP
authors.lastname: Kung
authors.forename: Hank F
authors.initials: HF
authors.lastname: Kung
authors.forename: Robert H
authors.initials: RH
authors.lastname: Mach
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000175:diagnosis*; D005260:Female; D005462:Fluorine Radioisotopes / Q000378:metabolism; D007457:Iodine Radioisotopes / Q000378:metabolism; D008024:Ligands; D049268:Positron-Emission Tomography; D011817:Rabbits; D051381:Rats; D017480:Receptors, sigma / Q000378:metabolism*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D005462:Fluorine Radioisotopes; D007457:Iodine Radioisotopes; D008024:Ligands; D017480:Receptors, sigma; C106107:sigma-2 receptor