Distribution of 16alpha-[18F]fluoro-estradiol-3,17beta-disulfamate in rats, tumour-bearing mice and piglets.
Based on a high affinity to the enzyme estrone sulfatase (ES), 16alpha-[18F]fluoroestradiol-3,17beta-disulfamate ([18F]FESDS) has been suggested as a potential PET radiotracer for imaging steroid-dependent breast tumours. The distribution of [18F]FESDS was studied in rats, tumour-bearing nude mice and piglets. In all species evidence for binding to a second target, the enzyme carbonic anhydrase (CA), was obtained. ES and CA inhibitors significantly reduced the radiotracer uptake in various organs but not in tumours. It is concluded that [18F]FESDS binds to ES and CA in vivo but this binding is not strong enough to allow tumour imaging with positron emission tomography (PET).
Brust
P
P
Forschungszentrum Rossendorf, Dresden, Germany. brust@iif-leipzig.de
Rodig
H
H
Römer
J
J
Kasch
H
H
Bergmann
R
R
Füchtner
F
F
Zips
D
D
Baumann
M
M
Steinbach
J
J
Johannsen
B
B
D000818:Animals; D001943:Breast Neoplasms / Q000000981:diagnostic imaging; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D005260:Female; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D013552:Swine; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured
C441859:16-fluoroestradiol-3,17-disulfamate; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D004958:Estradiol