1. Distribution of 16α-[18F]fluoro-estradiol-3,17β-disulfamate in rats, tumour-bearing mice and piglets
- Author
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Brust, P., Rodig, H., Römer, J., Kasch, H., Bergmann, R., Füchtner, F., Zips, D., Baumann, M., Steinbach, J., and Johannsen, B.
- Subjects
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CARBONIC anhydrase , *FLUORINE isotopes , *SULFATASES - Abstract
Based on a high affinity to the enzyme estrone sulfatase (ES), 16α-[18F]fluoroestradiol-3,17β-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). [Copyright &y& Elsevier]
- Published
- 2002
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