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.
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.
Tu
Zhude
Z
Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 South Kingshighway Blvd., St. Louis, MO 63110, USA.
Xu
Jinbin
J
Jones
Lynne A
LA
Li
Shihong
S
Zeng
Dexing
D
Kung
Mei-Ping
MP
Kung
Hank F
HF
Mach
Robert H
RH
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
D005462:Fluorine Radioisotopes; D007457:Iodine Radioisotopes; D008024:Ligands; D017480:Receptors, sigma; C106107:sigma-2 receptor